Contents

1 2025
2 2024
3 2023
4 2022
5 2021
6 2020
7 2019
8 2018
9 2017
10 2016
11 2015
12 2014
13 2013

2025

561. Garhwal, S.; Kutateladze, D. A.; Mai, B. K.; Dong, Y.; Liu, P. and Buchwald, S. L. “Copper Hydride-Catalyzed Net Hydroformylation of Unactivated Terminal Olefins.” Org. Lett. 2025, 27, 8747–8751.

560. Ha, S. K.; Kalyani, D.; West, M. S.; Xu, J.; Lam, Y.-H. Struble, T.; Dreher, S.; Krska, S. W.; Buchwald, S. L. and Jensen, K. G. “Developing Pharmaceutically Relevant Pd-Catalyzed C–N Coupling Reactivity Models Leveraging High-Throughput Experimentation.” J. Am. Chem. Soc. 2025, 147, 19602-19613.

559. Fittolani, G.; Kutateladze, D. A.; Loas, A.; Buchwald, S. L. and Pentelute, B. L. “Automated Flow Synthesis of Artificial Heme Enzymes for Enantiodivergent Biocatalysis.” J. Am. Chem. Soc. 2025, 147, 4188-4197.

2024

558. Raguram, E. R.; Dahl, J. C.; Jensen, K. F. and Buchwald, S. L. “Kinetic Modeling Enables Understanding of Off-Cycle Processes in Pd-Catalyzed Amination of Five-Membered Heteroaryl Halides.” J. Am. Chem. Soc. 2024, 146, 33035-33047.

557. Ai, H.-J.; Kim, S.-T.; Liu, C. and Buchwald, S.L. “Copper-Catalyzed Amination of Aryl Chlorides Under Mild Reaction Conditions.” J. Am. Chem. Soc. 2024, 146, 25949-25955.

556. Feng, K.; Raguram, E.R.; Howard, J.R.; Peters, E.; Liu, C.; Sigman, M.S. and Buchwald, S.L. “Development of a Deactivation-Resistant Dialkylbiarylphosphine Ligand for Pd-Catalyzed Arylation of Secondary Amines.” J. Am. Chem. Soc. 2024, 146, 26609-26615.

555. Tao, J.; Dhanjee, H.H.; Gribble, Jr., M.W.; Kottisch, V.; Rodriguez, J.; Brown, J.S.; Schmidt, H.; Juneja, J.; Denhez, F.; Lee, P.S.; Lipovšek, D.; Krystek, S.; Zhang, Y.; Bousquet, P.; Zhang, Y.; Petelute, B.L. and Buchwald, S.L. “Site-Specific Antibody Prodrugs via S-Arylation; A Bioconjugation Approach Toward Masked Tyrosine Analogues.” J. Am. Chem. Soc. 2024, 146, 20080-20085.

554. Strauss, M.J.; Liu, K.X.: Greaves, M.E.; Dahl, J.C.: Kim, S.-T.; Wu, Y.-J.; Schmidt, M.A.; Scola, P.M. and Buchwald, S.L. “Cu-Catalyzed Amination of Base-Sensitive Aryl Bromides and the Chemoselective N– and O-Arylation of Amino Alcohols.” J. Am. Chem. Soc. 2024, 146, 18616-18625.

553. Garhwal, S.; Dong, Y.; Mai, B.K.; Liu, P. and Buchwald, S.L. “CuH-Catalyzed Regio- and Enantioselective Formal Hydroformylation of Vinyl Arenes.” J. Am. Chem. Soc. 2024, 146, 13733-13740.

552. Strauss, M.J.; Greaves, M.E.; Kim, S.-T.; Teijaro, C.N.; Schmidt, M.A.; Scola, P.M. and Buchwald, S.L. “Room-Temperature Copper-Catalyzed Etherification of Aryl Bromides.” Angew. Chem. Int. Ed. 2024, 63, e202400333.

551. Grob, N.; Remarcik, C.; Rössler, S.; Wong, J.; Wang, J.; Tao, J.; Smith, C.; Loas, A.; Buchwald, S.L.; Eaton, D.; Preciado López, M. and Pentelute, B.L. “Electrophile Scanning Reveals Reactivity Hotspots for the Design of Covalent Peptide Binders.” ACS Chem. Biol. 2024, 19, 101-109.

2023

550. Kutateladze, D.; Mai, B.K.; Dong, Y.; Zhang, Y.; Liu, P. and Buchwald, S.L. “Stereoselective Synthesis of Trisubstituted Alkenes via Copper Hydride-Catalyzed Alkyne Hydroalkylation.” J. Am. Chem. Soc. 2023, 145, 17557-17563.

549. Kim, S.-T.; Strauss, M.J.; Cabré, A. and Buchwald, S.L. “Room Temperature Cu-Catalyzed Amination of Aryl Bromides Enabled by DFT-Guided Ligand Design.” J. Am. Chem. Soc. 2023,145, 6966-6975.

548. Ye, Y.; Kim, S.-T.; King, R.P.; Baik, M.-H. and Buchwald, S.L. “Studying Regioisomer Formation in the Pd-Catalyzed Fluorination of Cyclic Vinyl Triflates: Evidence for in situ Ligand Modification.” Angew. Chem. Int. Ed. 2023, 62, e202300109.

547. Reichert, E.C.; Feng, K.; Sather, A.C. and Buchwald, S.L. “Pd-Catalyzed Amination of Base-Sensitive Five-Membered Heteroaryl Halides with Aliphatic Amines.” J. Am. Chem. Soc. 2023,145, 3323-3329.

546. Rössler, S.L.; Grob, N.M.; Buchwald, S.L. and Pentelute, B.L. “Abiotic Peptides as Carriers of Information for the Encoding of Small Molecule Library Synthesis.” Science, 2023, 379, 939-946.

2022

545. Knippel, J.L.; Ni, A.Z.; Schuppe, A.W. and Buchwald, S.L. “A General Strategy for the Asymmetric Preparation of α-Stereogenic Allyl Silanes, Germanes, and Boronate Esters via Dual Copper Hydride- and Palladium-Catalysis.” Angew. Chemie. Int. Ed., 2022 61, e202212630.

544. Rojas, A.J.; Wolfe, J.M.; Dhanjee, H.H.; Buslov, I.; Truex, N.L.; Liu, R.Y.; Massefski, W.; Pentelute, B.L. and Stephen L. Buchwald. “Palladium-Peptide Oxidative Addition Complexes for Bioconjugation.” Chem. Sci., 2022, 13, 11891-11895.

543. Dong, Y.; Shin, K.; Mai, B.K.; Liu, P. and Buchwald, S.L. “Copper Hydride-Catalyzed Enantioselective Olefin Hydromethylation.” J. Am. Chem. Soc. 2022, 144, 36, 16303-16309.

542. Rodriguez, J.; Dhanjee, H.H.; Buchwald, S.L. and Pentelute, B.L. “Palladium Mediated Synthesis of Protein-Polyarene Conjugates.” J. Am. Chem. Soc. 2022, 144, 11706.

541. Feng, S. and Buchwald, S.L. “Enantioselective Hydrocarbamoylation of Alkenes.” Angew. Chem. Int. Ed. 2022, 61, e202206692.

540. Gazvoda, M.; Dhanjee, H.H.; Rodriguez, J.; Brown, J.S.; Farquhar, C.E.; Truex, N.L.; Loas, A.; Buchwald, S.L. and Pentelute, B.L. “Palladium-Mediated Incorporation of Carboranes into Small Molecules, Peptides, and Proteins.” J. Am. Chem. Soc. 2022, 144, 7852-7860.

539. Dong, Y.; Schuppe, A.W.; Mai, B.K.; Liu, P. and Buchwald, S.L. “Confronting the Challenging Asymmetric Carbonyl 1,2-Addition using Vinyl Heteroarene Pronucleophiles: Ligand-Controlled Regiodivergent Processes Through a Dearomatized Allyl-Cu Species.” J. Am. Chem. Soc. 2022, 144, 5985-5995.

2021

538. Hou,C.-J.; Schuppe, A.W.; Knippel, J.L.; Ni, A.Z. and Buchwald, S.L. “A Dual CuH- and Pd-Catalyzed Stereoselective Synthesis of Highly Substituted 1,3-Dienes.” Org. Lett. 2021, 23, 8816-8821.

537. King, R.P.; Krska, S.W. and Buchwald, S.L. “A Neophyl Palladacycle as an Air- and Thermally Stable Precursor to Oxidative Addition Complexes.” Org. Lett. 2021, 23, 7927–7932.

536. King, R.P.; Krska, S.W. and Buchwald, S.L. “A Ligand Exchange Process for the Diversification of Palladium Oxidative Addition Complexes.” Org. Lett. 2021, 23, 6030-6034.

535. Jbara, M.; Pomplun, S.; Schissel, C.K.; Wilson-Hawken, S.; Boija, A.; Klein, I.; Rodriguez, J.; Buchwald, S.L. and Pentelute, B.L. “Engineering Bioactive Dimeric Transcription Factor Analogs via Palladium Rebound Reagents.” J. Am. Chem. Soc. 2021, 143, 11788-11798.

534. Mallek, A.J.; Pentelute, B.L. and Buchwald, S.L. “Selective N-Arylation of p-Aminophenylalanine in Unprotected Peptides with Organometallic Palladium Reagents.” Angew. Chem. Int. Ed. 2021, 60, 16928-16931.

533. Schuppe, A.W.; Knippel, J.L.; Borrajo-Calleja, G.M. and Buchwald, S.L. “Enantioselective Hydroalkenylation of Olefins with Enol Sulfonates Enabled by Dual Copper Hydride and Palladium Catalysis.” J. Am. Chem. Soc. 2021,143, 5330-5335.

532. Feng, S. and Buchwald, S.L. “CuH-Catalyzed Regio- and Enantioselective Hydrocarboxylation of Allenes: Towards Carboxylic Acids with Acyclic Quaternary Centers.” J. Am. Chem. Soc. 2021,143, 4935-4941.

531. Jbara, M.; Rodriguez, J.; Dhanjee, H.H.; Loas, A.; Buchwald, S.L. and Pentelute, B.L. “Oligonucleotide Bioconjugation with Bifunctional Palladium Reagents.“ Angew. Chem. Int. Ed. 2021, 60, 12109-12115.

530. Knippel, J.L.; Ye, Y. and Buchwald, S.L. “Enantioselective C2-Allylation of Benzimidazoles Using 1,3-Diene Pronucleophiles.” Org. Lett. 2021, 23, 2153-2157.

529. Rodriguez, J.; Dhanjee, H.H. and Buchwald, S.L. “Amphiphilic Biaryl Monophosphine Ligands by Regioselective Sulfonation.” Org. Lett. 2021, 33, 777-780.

2020

528. Dhanjee, H.H.; Buslov, I.; Windsor, I.W.; Pentelute, B.L. and S.L. Buchwald. “Palladium–Protein Oxidative Addition Complexes by Amine-Selective Acylation.” J. Am. Chem. Soc. 2020, 142, 21237-21242.

527. McCann, S.D.; Reichert, E.C.; Arrechea, P.L. and Buchwald, S.L. “Development of an Aryl Amination Catalyst with Broad Scope Guided by Consideration of Catalyst Stability.” J. Am. Chem. Soc. 2020, 142, 15027-15037.

526. Link, A.; Zhou, Y. “CuH-Catalyzed Asymmetric Reductive Amidation of α,β-Unsaturated Carboxylic Acids.” Org. Lett. 2020, 22, 5666-5670.

525. Guo, S.; Zhu, J. and Buchwald, S.L. “Enantioselective Synthesis of β-Amino Acid Derivatives Enabled by Ligand-Controlled Reversal of Hydrocupration Regiochemistry.” Angew. Chem. Int. Ed. 2020, 59, 20841–20845.

524. Zhang, H.; Ruiz-Castillo, P.; Schuppe, A.W. and Buchwald, S.L. “Palladium-Catalyzed C–O Cross-Coupling of Secondary Alcohols.” Org. Lett. 2020, 22, 5369-5374.

523. Gribble, M. W.; Liu, R.Y. and Buchwald, S.L. “Evidence for Simultaneous Dearomatization of Two Arenes Under Mild Conditions in Cu(I)-Catalyzed Direct Asymmetric Dearomatization of Pyridine.” J. Am. Chem. Soc. 2020, 142, 11252-11269.

522. Lu, Z. and Buchwald, S.L. “The Enantioselective Preparation of Arenes with β-Stereogenic Centers: Confronting the 1,1-Disubstituted Olefin Problem Using CuH/Pd Cooperative Catalysis.” Angew. Chem. Int. Ed. 2020, 59, 16128-16132.

521. Ye, Y.; Jesikiewicz, L.T.; Feng, S.; Liu, P. and Buchwald, S.L. “Highly Enantioselective Synthesis of Indazoles with a C3-Quaternary Chiral Center Using CuH Catalysis.” J. Am. Chem. Soc. 2020, 142, 10550-10556.

520. Zhou, Y.; Zhou, L.; Jesikiewicz, L.T.; Liu, P. and Buchwald, S.L. “Synthesis of Pyrroles Through the CuH-Catalyzed Coupling of Enynes and Nitriles.” J. Am. Chem. Soc. 2020, 142, 9908-9914.

519. Dhanjee, H.H.; Saebi,A.; Buslov,I.; Loftis, A.R.; Buchwald, S.L. and Pentelute, B.L. “Protein-Protein Cross-Coupling via Palladium-Protein Oxidative Addition Complexes from Cysteine Residues.” J. Am. Chem. Soc. 2020, 142, 9124-9129.

518. Liu, R.Y. and Buchwald, S.L. “CuH-Catalyzed Olefin Functionalization: from Hydroamination to Carbonyl Addition.” Acc. Chem. Res. 2020, 53, 1229-1243.

517. Mo, Y.: Lu, Z.; Rughoobur, G.; Patil, P.; Gershenfeld, N.; Akinwande, A.I.; Buchwald, S.L. and Jensen, K.F. “Microfluidic electrochemistry for single-electron transfer redox-neutral reactions.” Science 2020, 368, 1352-1357.

GRAPHIC: C. BICKEL/SCIENCE

516. Liu, R.Y.; Dennis, J.M. and Buchwald, S.L. “The Quest for the Ideal Base: Rational Design of a Nickel Precatalyst Enables Mild, Homogeneous C–N Cross-Coupling.” J. Am. Chem. Soc. 2020, 142, 4500-4507.

515. Park, B.Y.; Pirnot, M.T. and Buchwald, S.L. “Visible Light-Mediated (Hetero)aryl Amination Using Ni(II) Salts and Photoredox Catalysis in Flow: A Synthesis of Tetracaine.” J. Org. Chem. 2020, 85, 3234-3244.

514. Feng, S.; Hao, H.; Liu, P. and Buchwald, S.L. “Diastereo- and Enantioselective CuH-Catalyzed Hydroamination of Strained Trisubstituted Alkenes.” ACS Catal. 2020, 10, 282-291.

2019

513. Schuppe, A.W.; Borrajo-Calleja, G.M. and Buchwald, S.L. “Enantioselective Olefin Hydrocyanation Without Cyanide.” J. Am. Chem. Soc. 2019, 141, 18668-18672.

512. Ichikawa, S. and Buchwald, S.L. “Asymmetric Synthesis of γ-Amino Alcohols by Copper-Catalyzed Hydroamination.” Org. Lett. 2019, 21, 8736-8739.

511. Li, C.; Shin, K.; Liu, R.Y. and Buchwald, S.L. “Engaging Aldehydes in CuH-Catalyzed Reductive Coupling Reactions: Stereoselective Allylation with Unactivated 1,3-Diene Pronucleophiles.” Angew. Chem. Int. Ed. 2019, 58, 17074-17080.

510. King, R.P. and Buchwald, S.L. “Synthesis of (MeCN)₂Pd(CF₃)OTs, a General Precursor to Palladium(II)–Trifluoromethyl Complexes LPd(CF3)X.” Organometallics 2019, 38, 3490-3493.

509. Wagen, C.C.; Ingoglia, B.T. and Buchwald, S.L. “Unexpected Formation of Hexasubstituted Arenes through a Twofold Palladium-Mediated Ligand Arylation.” J. Org. Chem. 2019, 84, 12672-12679.

508. Bayeh-Romero, L. and Buchwald, S.L. “Copper Hydride-Catalyzed Enantioselective Synthesis of Axially Chiral 1,3-Disubstituted Allenes.” J. Am. Chem. Soc. 2019, 141, 13788-13794.

507. Huang, W.; Einzinger, M.; Maurano, A.; Zhu, T.; Tiepelt, J.; Chae, H.S.; Van Voorhis, T.; Baldo, M.A. and Buchwald, S.L. “Large Increase in External Quantum Efficiency by Dihedral Angle Tuning in a Sky-Blue Thermally Activated Delayed Fluorescence Emitter.” Adv. Optical Mater. 2019, 7, 1900476.

506. Baumgartner, L.M.; Dennis, J.M.; White, N.A.; Buchwald, S.L. and Jensen, K.F. “Use of a Droplet Platform to Optimize Pd-Catalyzed C−N Coupling Reactions Promoted by Organic Bases.” Org. Process Res. Dev. 2019, 23, 1594-1601.

505. Xu, J.; Liu, R.Y.; Yeung, C.S. and Buchwald, S.L. “Monophosphine Ligands Promote Pd-Catalyzed C–S Cross-Coupling Reactions at Room Temperature with Soluble Bases.” ACS Catal. 2019, 9, 6461-6466.

504. Ichikawa, S.; Dai, X.-J. and Buchwald, S.L. “Regio- and Enantioselective Synthesis of 1,2-Diamine Derivatives by Copper-Catalyzed Hydroamination.” Org. Lett. 2019, 21, 4370-4373.

503. Ingoglia, B.T.: Wagen, C.C. and Buchwald, S.L. “Biaryl Monophosphine Ligands in Palladium-Catalyzed C-N Coupling: An Updated User’s Guide.” Tetrahedron 2019, 75, 4199–4211.

502. Dennis, J. M. ; White, N. A. ; Liu, R. Y. and Buchwald, S. L. “Pd-Catalyzed C–N Coupling Reactions Facilitated by Amine Bases: Mechanistic Investigation Leads to Enhanced Reactivity in the Arylation of Weakly Binding Amines.” ACS Catal. 2019, 9, 3822 – 3830.

501. Li,C.; Liu, R.Y.; Jesikiewicz, L.T.; Yang, Y.; Liu, P. and Buchwald, L. “CuH-Catalyzed Enantioselective Ketone Allylation with 1,3-Dienes: Scope, Mechanism, and Applications.” J. Am. Chem. Soc. 2019, 141, 5062-5070.

500. Ye, Y.; Kim, S.-T.; Jeong, J.; Baik, M.-H. and Buchwald, S.L. “CuH-Catalyzed Enantioselective Alkylation of Indole Derivatives with Ligand-Controlled Regiodivergence.” J. Am. Chem. Soc. 2019, 141, 3901-3909.

499. Liu, R.Y.; Zhou, Y.; Yang, Y. and Buchwald, S.L. “Enantioselective Allylation from Allene, a Petroleum Cracking Byproduct.” J. Am. Chem. Soc. 2019, 141, 2251-2256.

498. Dai, X.-J.; Engl, O.D. and Buchwald, S.L. “Catalytic Asymmetric Synthesis of α-Arylpyrrolidines and Benzo-fused Nitrogen Heterocycles.” Angew. Chem. Int. Ed. 2019, 58, 3407-3411.

497. Uehling, M.R.; King, R.P.; Krska, S. W.; Cernak, T. and Buchwald, S.L. “Pharmaceutical Diversification via Palladium Oxidative Addition Complexes.” Science, 2019, 363, 405-408.

496. Zhang, C.; Vinogradova, E.; Spokoyny, A.; Buchwald, S.L. and Pentelute, B.L. “Arylation Chemistry for Bioconjugation.” Angew. Chem. Int. Ed. 2019, 58, 4810-4839.

495. Cohen, D.T.; Zhang, C.; Fadzen, C.M.; Mijalis, A.J.; Hie, L.; Johnson, K.D.; Shriver, Z.; Plante, O.; Miller, S.J.; Buchwald, S.L. and Pentelute, B.L. “A Chemoselective Strategy for Late Stage Functionalization of Complex Small Molecules with Polypeptides and Proteins.” Nature Chem. 2019, 11, 78-85.

2018

494. Guo, S.; Yang, J.C. and Buchwald, S.L. “A Practical Electrophilic Nitrogen Source for the Synthesis of Chiral Primary Amines by Copper-Catalyzed Hydroamination.” J. Am. Chem. Soc. 2018, 140, 15976-15984.

493. Thomas, A.A.; Speck, K.; Kevlishvili, I.; Lu, Z.; Liu, P. and Buchwald, S.L. “Mechanistically Guided Design of Ligands that Significantly Improve the Efficiency of CuH-Catalyzed Hydroamination Reactions.” J. Am. Chem. Soc. 2018, 140, 13976-13984.

492. Khan, R.K.M.; Zhao, Y.; Scully, T.D. and Buchwald S.L. “Catalytic Arylhydroxylation of Dehydroalanine in Continuous Flow for Simple Access to Unnatural Amino Acids.” Chem. Eur. J. 2018, 24, 15215.

491. Ichikawa, S.; Zhu, S. and Buchwald, S.L. “A Modified System for the Synthesis of Enantioenriched N-Arylamines through Copper-Catalyzed Hydroamination.” Angew. Chem. Int. Ed. 2018, 57, 8714-8718.

490. Liu, R.Y. and Buchwald, S.L. “Copper-Catalyzed Enantioselective Hydroamination of Alkenes.” Org. Syn. 2018, 95, 80-96.

489. Zhou, Y.; Engl, O.D.; Bandar, J.S.; Chant, E.D. and Buchwald, S.L. “CuH-Catalyzed Asymmetric Hydroamidation of Vinylarenes.” Angew. Chem. Int. Ed. 2018, 57, 6672-6675.

488. Gribble, M.W.; Guo, S. and Buchwald, S.L. “Asymmetric Cu-Catalyzed 1,4-Dearomatization of Pyridines and Pyridazines without Preactivation of the Heterocycle or Nucleophile.” J. Am. Chem. Soc. 2018, 140, 5057-5060.

487. Dennis, J.M.; White, N.A.; Liu, R.Y. and Buchwald, S.L. “Breaking the Base Barrier: An Electron-Deficient Palladium Catalyst Enables the Use of a Common, Soluble Base in C–N Coupling.” J. Am. Chem. Soc. 2018, 140, 4721-4725.

486. Zhang, H.; Ruiz-Castillo, P. and Buchwald, S.L. “Palladium-Catalyzed C–O Cross-Coupling of Primary Alcohols.” Org. Lett. 2018, 20, 1580-1583.

485. Huang, W.; Einzinger, M.; Zhu, T.; Chae, H.S.; Jeon, S.; Ihn, S.-G.; Sim, M.; Kim, S.; Teverovskiy, G.; Wu, T.; Van Voorhis, T.; Swager, T.M.; Baldo, M.A. and Buchwald, S.L. “Molecular Design of Deep Blue Thermally Activated Delayed Fluorescence Materials Employing a Homoconjugative Triptycene Scaffold and Dihedral Angle Tuning.” Chem. Mater. 2018, 30, 1462-1466.

484. Kubota,K.; Dai,P.; Pentelute, B.L. and Buchwald, S.L. “Palladium Oxidative Addition Complexes for Peptide and Protein Crosslinking.” J. Am. Chem. Soc. 2018, 140, 3128-3133.

483. Tsai, E.Y.; Liu, R. Y. and Buchwald, S.L. “A Regio- and Enantioselective CuH-Catalyzed Ketone Allylation with Terminal Allenes.” J. Am. Chem. Soc. 2018, 140, 2007-2011.

482. Liu, R. Y.; Bae, M. and Buchwald, S.L. “Mechanistic Insight Facilitates Discover of a Mild and Efficient Copper-Catalyzed Dehydration of Primary Amides.” J. Am. Chem. Soc. 2018, 140, 1627-1631.

481. Zhou, Y.; Bandar, J.S.; Liu, R.Y. and Buchwald, S.L. “CuH-Catalyzed Asymmetric Reduction of α,β-Unsaturated Carboxylic Acids to β-Chiral Aldehydes.” J. Am. Chem. Soc. 2018, 140, 606-609.

2017

480. Lu, G.; Liu, R.L.; Yang, Y.; Fang, C.; Lambrecht, D.S.; Buchwald S.L. and Liu, P. “Ligand-Substrate Dispersion Facilitates the Copper-Catalyzed Hydroamination of Unactivated Olefins.” J. Am. Chem. Soc. 2017, 139, 16548-16555.

479. Rojas, A.J.; Pentelute, B.L. and Buchwald, S.L. “Water-Soluble Palladium Reagents for Cysteine S-Arylation Under Ambient Aqueous Conditions.” Org. Lett. 2017, 19, 4263-4266.

478. Zhang, H. and Buchwald, S.L. “Palladium-Catalyzed Negishi Coupling of α-CF₃ Oxiranyl Zincate: Access to Chiral CF₃-substituted Benzylic Tertiary Alcohols” J. Am. Chem. Soc. 2017, 139, 11590-11594.

477. Olsen, E.P.K.; Arrechea, P.L. and Buchwald, S.L. “Mechanistic Insight Leads to a New Ligand That Facilitates the Pd-Catalyzed Formation of 2-(Hetero)Arylaminooxazoles and 4-(Hetero)Arylaminothiazoles.” Angew. Chem. Int. Ed. 2017, 56, 10569-10572.

476. Wang, H.; Yang, J.C. and Buchwald, S.L. “CuH-Catalyzed Regioselective Intramolecular Hydroamination for the Synthesis of Alkyl-Substituted Chiral Aziridines.” J. Am. Chem. Soc. 2017, 139, 8428-8431.

475. Zhou, Y.; Bandar, J.S. and Buchwald, S.L. “Enantioselective CuH-Catalyzed Hydroacylation Employing Unsaturated Carboxylic Acids as Aldehyde Surrogates.” J. Am. Chem. Soc. 2017, 139, 8126-8129.

474. Zhao, W.; Lee, H.G.; Buchwald, S.L. and Hooker, J.M. “Direct ¹¹CN-Labeling of Unprotected Peptides via Palladium-Mediated Sequential Cross-Coupling Reactions.” J. Am. Chem. Soc. 2017, 139, 7152-7155.

473. Ingoglia, B.T. and Buchwald, S.L. “Oxidative Addition Complexes as Precatalysts for Cross-Coupling Reactions Requiring Extremely Bulky Biarylphosphine Ligands.” Org. Lett. 2017, 19, 2853-2858.

472. Friis, S.D.; Pirnot, M.T.; Dupuis, L.N. and Buchwald, S.L. “A Dual Pd- and CuH-Catalyzed Approach for Alkyl-Aryl Cross-Coupling of Aryl Halides and Olefins.” Angew. Chem. Int. Ed. 2017, 56, 7242-7246.

471. Rojas, A.J.; Zhang, C.; Vinogradova, E.V.; Buchwald, N.H.; Reilly, J.; Pentelute, B.L. and Buchwald, S.L. “Divergent Unprotected Peptide Macrocyclisation by Palladium-mediated Cysteine Arylation.” Chem. Sci. 2017, 8, 4257-4263.

470. Gribble, M.W.; Pirnot, M.T.; Bandar, J.S. and Buchwald, S.L. “Asymmetric Copper Hydride-Catalyzed Markovnikov Hydrosilylation of Vinylarenes and Vinyl Heterocycles.” J. Am. Chem. Soc. 2017, 139, 2192-2195.

469. Lee, H.G.; Lautrette, G.; Pentelute, B.L. and Buchwald, S.L. “Pd-Mediated Arylation of Lysine in Unprotected Peptides.” Angew. Chem. Int. Ed. 2017, 56, 3177-3181.

2016

468. Ye, Y.; Takeda, T. and Buchwald, S.L. “Palladium-Catalyzed Fluorination of Cyclic Vinyl Triflates: Effect of TESCF₃ as an Additive.” Angew. Chem. Int. Ed. 2016, 55, 15559-15563.

467. Liu, R.Y.; Yang, Y. and Buchwald, S.L. “CuH-Catalyzed Allylation of Imines from Terminal Allenes.” Angew. Chem. Int. Ed. 2016, 55, 14077-14080.

466. Reizman, B.J.; Wang, Y.-M.; Buchwald, S.L. and Jensen, K.F. “Suzuki– Miyaura Cross-coupling Optimization Enabled by Automated Feedback.” React. Chem. Eng. 2016 1, 658-666.

465. Ruiz-Castillo, P. and Buchwald, S.L. “Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions.” Chem. Rev. 2016, 116, 12564-12649.

464. Sather, A.C. and Buchwald, S.L. “The Evolution of Pd⁰/Pd^II-Catalyzed Aromatic Fluorination.” Acc. Chem. Res. 2016, 49, 2146-2157.

463. Arrechea, P.L. and Buchwald, S.L.“Biaryl Phosphine Based Pd(II) Amido Complexes: The Effect of Ligand Structure on Reductive Elimination.” J. Am. Chem. Soc. 2016, 138, 12486-12493.

462. Park, N.H.; Senter, T.J. and Buchwald, S.L. “Rapid Synthesis of Aryl Fluorides in Continuous Flow via the Balz-Schiemann Reaction.” Angew. Chem. Int. Ed 2016, 55, 11907-11911.

461. King, S.M. and Buchwald, S.L. “Development of a Method for the N-Arylation of Amino Acid Esters with Aryl Triflates.“ Org. Lett. 2016, 18, 4128-4131.

460. Yang, Y.; Perry, I.B. and Buchwald, S.L. “Copper-Catalyzed Enantioselective Addition of Styrene-Derived Nucleophiles to Imines Enabled by Ligand-Controlled Chemoselective Hydrocupration.” J. Am. Chem. Soc. 2016, 138, 9787-9790.

459. Huang, W. and Buchwald, S.L. “Palladium-catalyzed N-Arylation of Iminodibenzyls and Iminostilbenes with Aryl and Hetero-Aryl Halides.” Chem. Eur. J. 2016, 22, 14186-14189.

458. Vincent, B.M.; Langlois, J.-B.; Srinivas, R.; Lancaster, A.K.; Scherz-Shouval, R.; Whitesell, L.; Tidor, B.; Buchwald, S.L. and Lindquist, S.L. “A Fungal-Selective Cytochrome bc1 Inhibitor Impairs Virulence and Prevents the Evolution of Drug Resistance.” Cell Chemical Biology, 2016, 23, 978-991.

457. Friis, S.D.; Pirnot, M.T. and Buchwald, S.L. “Asymmetric Hydroarylation of Vinylarenes Using a Synergistic Combination of CuH and Pd Catalysis.” J. Am. Chem. Soc. 2016, 138, 8372-8375.

456. Roesner, S. and Buchwald, S.L. “Continuous Flow Synthesis of Biaryls by Negishi Cross-Coupling of Fluoro- and Trifluoromethyl-Substituted (Hetero)arenes.” Angew. Chem. 2016, 55, 10463-104637.

455. Corcoran, E.B.; Pirnot, M.T.; Lin, S.; Dreher, S.D.; DiRocco, D.A.; Davies, I.W., Buchwald, S.L. and MacMillan, D.W.C. “Aryl Amination Using Ligand-free Ni(II) Salts and Photoredox Catalysis.” Science, 2016, 353, 279-283.

454. Yang, Y.; Perry, I.B.; Lu, G.; Liu, P. and Buchwald, S.L. “Copper-Catalyzed Asymmetric Addition of Olefin-Derived Nucleophiles to Ketones.” Science, 2016, 353, 144-150.

453. Bandar, J.S. and Buchwald, S.L. “Enantioselective CuH-Catalyzed Reductive Coupling of Aryl Alkenes and Activated Carboxylic Acids.” J. Am. Chem. Soc. 2016, 138, 5821-5824.

452. Smith, S.M. and Buchwald, S.L. “Regioselective 2-Amination of Polychloropyrimidines.” Org. Lett. 2016, 18, 2180-2183.

451. Wang, Y.-M. and Buchwald, S.L. “Enantioselective CuH-Catalyzed Hydroallylation of Vinylarenes.” J. Am. Chem. Soc. 2016, 138, 5024-5027.

450. Shi, S.-L.; Wong, Z. and Buchwald, S.L. “Copper-catalyzed Enantioselective Stereodivergent Synthesis of Amino Alcohols.” Nature, 2016, 532, 353-356.

449. Yang, J.C.; Niu, D.; Karsten, B.P.; Lima, F. and Buchwald, S.L.“Use of a “Catalytic” Cosolvent, N,N-Dimethyl Octanamide, Allows the Flow Synthesis of Imatinib With No Solvent Switch.” Angew. Chem. Int. Ed. 2016, 55, 2531-2535.

448. Bhonde, V.R.; O’Neill, B.T. and Buchwald, S.L. “An Improved System for the Aqueous Lipshutz−Negishi Cross-Coupling of Alkyl Halides with Aryl Electrophiles.” Angew. Chem. Int. Ed. 2016, 55, 1849-1853.

447. Zhu, S.; Niljianskul, N. and Buchwald, S.L. “A Direct Approach To Amines With Remote Stereocenters By Enantioselective CuH-Catalysed Reductive Relay Hydroamination.” Nature Chem. 2016, 8, 144-150.

2015

446. Bandar, J.S.; Pirnot, M.T. and Buchwald, S.L. “Mechanistic Studies Lead to Dramatically Improved Reaction Conditions for the Cu-Catalyzed Asymmetric Hydroamination of Olefins.” J. Am. Chem. Soc. 2015, 137, 14812-14818.

445. Sather, A. C.; Lee, H. G.; De La Rosa, V. Y.; Yang, Y.; Müller, P.; Buchwald, S. L. “A Fluorinated Ligand Enables Room Temperature and Regioselective Pd-Catalyzed Fluorination of Aryl Triflates and Bromides.” J. Am. Chem. Soc. 2015, 137, 13433-13438.

444. Pirnot, M.T.; Wang, Y.-M. and Buchwald, S.L. “Copper Hydride-Catalyzed Hydroamination of Alkenes and Alkynes.” Angew. Chem. Int. Ed. 2016, 55, 48-57.

443. Vinogradova, E.V., Zhang, C.; Spokoyny, A.M.; Pentelute, Bradley L. and Buchwald, S.L. “Organometallic Palladium Reagents for Cysteine Bioconjugation.” Nature, 2015, 526, 687-691.

442. Milner, P.J.; Yang, Y. and Buchwald, S.L. “In-Depth Assessment of the Pd-Catalyzed Fluorination of 5-Membered Heteroaryl Bromides.” Organometallics, 2015, 34, 4775-4780.

441. Sather, A.C.; Lee, H.G.; Colombe, J.R.; Zhang, A. and Buchwald, S.L. “Dosage Delivery of Sensitive Reagents Enables Glove-Box-Free Synthesis.” Nature, 2015, 524, 208-211.

440. Wang, Y.-M.; Bruno, N.C.; Placeres, A.; Zhu, S. and Buchwald, S.L. “Enantioselective Synthesis of Carbo- and Heterocycles Through a CuH-Catalyzed Hydroalkylation Approach.” J. Am. Chem. Soc. 2015, 137, 10524-10527.

439. Cohen, D.T.; Zhang, C.; Pentelute, B.L. and Buchwald, S.L. “An Umpolung Approach for the Chemoselective Arylation of Selenocysteine in Unprotected Peptides.” J. Am. Chem. Soc. 2015, 137, 9784-9787.

438. Niu, D. and Buchwald, S.L. “The Design of Modified Amine Transfer Reagents Allows the Synthesis of α-Chiral Secondary Amines via CuH-Catalyzed Hydroamination.” J. Am. Chem. Soc. 2015, 137, 9716-9721.

437. Zhu, R. and Buchwald, S.L. “Versatile Enantioselective Synthesis of Functionalized Lactones via Copper-Catalyzed Radical Oxyfunctionalization of Alkenes.” J. Am. Chem. Soc. 2015, 137, 8069-8077.

436. Yang, Y.; Shi, S.; Niu, D.; Liu, P. and Buchwald, S.L. “Catalytic Asymmetric Hydroamination of Unactivated Internal Olefins to Aliphatic Amines.” Science, 2015, 349, 62-66.

435. Colombe, J.R.; DeBergh, J.R. and Buchwald, S.L. “Synthesis of Heteroaryl Sulfonamides from Organozinc Reagents and 2,4,6-Trichlorosulfate.” Org. Lett. 2015, 17, 3170-3173.

434. Park, N.H.; Vinogradova, E.V.; Surry, D.S. and Buchwald, S.L. “Design of New Ligands for the Palladium-Catalyzed Arylation of α-Branched Secondary Amines.” Angew. Chem. Int. Ed. 2015, 54, 8259-8262.

433. Asic, E. and Buchwald, S.L. “Highly Diastereo- and Enantioselective CuH-Catalyzed Synthesis of 2,3-Disubstituted Indolines.” J. Am. Chem. Soc. 2015, 137, 4666-4669.

432. Ruiz-Castillo, P.; Blackmond, D.G. and Buchwald, S.L. “Rational Ligand Design for the Arylation of Hindered Primary Amines Guided by Reaction Progress Kinetic Analysis.” J. Am. Chem. Soc. 2015, 137, 3085-3092.

431. Lee, H.-G.; Milner, P.J.; Placzek, M.S.; Buchwald, S.L. and Hooker, J.M. “Virtually Instantaneous, Room-temperature [¹¹C]-Cyanation Using Biaryl Phosphine Pd(0) Complexes.” J. Am. Chem. Soc. 2015, 137, 648-651.

430. Cohen D.T. and Buchwald S.L. “Mild Palladium-Catalyzed Cyanation of (Hetero)aryl Halides and Triflates in Aqueous Media” Org. Lett. 2015, 17, 202-205.

429. Shi S. and Buchwald S.L. “Palladium-Catalyzed Intramolecular C-H Difluoroalkylation: Synthesis of Substituted 3,3-Difluoro-2-oxindoles” Angew Chem., Int. Ed. 2015, 54, 1646-1650.

428. Shi S.and Buchwald, S.L. “Copper-Catalysed Selective Hydroamination Reactions Of Alkynes.” Nature Chem. 2015, 7, 38-44.

427. Nilijiansku, N.; Zhu, S.and Buchwald, S.L. “Enantioselective Synthesis of α-Aminosilanes by Copper-Catalyzed Hydroamination of Vinylsilanes.“ Angew Chem. Int. Ed. 2015, 54, 1638-1641.

2014

426. Zhu, S. and Buchwald S.L. “Enantioselective CuH-Catalyzed Anti-Markovnikov Hydroamination of 1,1-Disubstituted Alkenes.” J. Am. Chem. Soc. 2014, 136, 15913 – 15916.

425. Chen, M; Ichikawa, S. and Buchwald S.L. “Rapid and Efficient Copper-Catalyzed Finkelstein Reaction of (Hetero)Aromatics under Continuous-Flow Conditions.“ Angew Chem. Int. Ed. 2014, 54, 263 – 266.

424. Milner, P.J.; Kinzel, T.; Zhang, Y. and Buchwald S.L. “Studying Regiosomer Formation in the Pd-Catalyzed Fluorination of Aryl Triflates by Deuterium Labeling.” J. Am. Chem. Soc. 2014, 36, 15757–15766.

423. Yang, Y.; Niedermann, K.; Han, C. and Buchwald, S.L. “Highly Selective Palladium-Catalyzed Cross-Coupling of Secondary Alkylzinc Reagents with Heteroaryl Halides.” Org. Lett. 2014, 16, 4638–4641.

422. Friis, S.D.; Skrydstrup, T. and Buchwald, S.L. “Mild Pd-Catalyzed Aminocarbonylation of (Hetero)Aryl Bromides with a Palladacycle Precatalyst.” Org. Lett. 2014, 16, 4296–4299.

421. Ernst, J.B.; Tay, N.E.S.; Jui, N.T. and Buchwald, S.L. “Regioselective Synthesis of Benzimidazolones via Cascade C–N Coupling of Monosubstituted Ureas.” Org. Lett. 2014, 16, 3844–3846.

420. Lee, H.G.; Milner, P.J.; Colvin, M.T.; Andreas, L. and Buchwald, S.L. “Structure and Reactivity of [(L•Pd)_n•(1,5-cyclooctadiene)] (n=1-2) Complexes Bearing Biaryl Phosphine Ligands.” Inorg. Chem. Acta. 2014, 422, 188-192.

419. Cheung, C.W. and Buchwald, S.L. “Palladium-Catalyzed Hydroxylation of Aryl and Heteroaryl Halides Enabled by the Use of a Palladacycle Precatalyst.” J. Org. Chem. 2014, 79, 5351-5358.

418. Bruno, N.C.; Niljianskul, N. and Buchwald, S.L. “N-Substituted 2-Aminobiphenylpalladium Methanesulfonate Precatalysts and their Use in C-C and C-N Cross-Couplings.” J. Org. Chem. 2014, 79, 4161-4166.

417. Yang, Y. and Buchwald, S.L. “Copper-Catalyzed Regioselective ortho C–H Cyanation of Vinylarenes.” Angew. Chem. Int. Ed. 2014, 126, 8821-8825.

416. Zhu, Y. and Buchwald, S.L. “Ligand-Controlled Asymmetric Arylation of Aliphatic α-Amino Anion Equivalents.” J. Am. Chem. Soc. 2014, 136, 4500-4503.

415. Lee, H.G.; Milner, P.J.; Buchwald, S.L. “Pd-Catalyzed Nucleophilic Fluorination of Aryl Bromides.” J. Am. Chem. Soc. 2014, 136, 3792-3795.

414. Su, M.; Hoshiya, N. and Buchwald, S.L. “Palladium-Catalyzed Amination of Unprotected Five-Membered Heterocyclic Bromides.” Org. Lett. 2014, 16, 832-835.

413. Vinogradova, E.V.; Müller, P. and Buchwald, S.L. “Structural Reevaluation of the Electrophilic Hypervalent Iodine Reagent for Trifluoromethylthiolation Supported by the Crystalline-Sponge Method for X-ray Analysis.” Angew. Chem. Int. Ed. 2014, 53, 3125-3128.

412. Park, N.H.; Teverovskiy, G. and Buchwald, S.L. “Development of an Air-Stable Nickel Precatalyst for the Amination of Aryl Chlorides, Sulfamates, Mesylates, and Triflates.” Org. Lett. 2014, 16, 220-223.

2013

411. Chung, C. Y.; Khurana, V.; Auluck, P. K.; Tardiff, D. F.; Mazulli, J. R.; Soldner, F.; Baru, V.; Lou, Y.; Freyzon, Y.; Cho, S.; Mungenast, A. E.; Muffat, J.; Mitalopoa, M.; Pluth, M. D.; Jui, N. T.; Schüle, B.; Lippard, S. L.; Tsai, L.-H.; Krainc, D.; Buchwald, S. L.; Jaenisch, R. and Lindquist, S. “Identification and Rescue of α-Synuclein Toxicity in Parkinson Patient Neurons.” Science 2013, 342, 983-987.

410. Tardiff, D. F.; Jui, N. T.; Khurana, V.; Tambe, M. A.; Thompson, M. L.; Chung, C. Y. Kamadurai, H.; Kim, H.-T.; Lancaster, A. K.; Caldwell, K. A.; Caldwell, G. A.; Rochet, J.-C.; Buchwald, S. L. and Lindquist, S. “Yeast Reveal a “Druggable” Rsp5/Nedd4 Network that Ameliorates α-Synuclein Toxicity.” Science 2013, 342, 979-983.

409. Colombe, J.R.; Bernhardt, S.; Stathakis, C.; Buchwald, S.L. and Knochel, P. “Synthesis of Solid 2-Pyridylzinc Reagents and their Application in Negishi Reactions.” Org. Lett. 2013, 15, 5754-5757.

408. Yang, Y.; Mustard, T.J.L.; Cheong, P.H.-Y. and Buchwald, S.L. “Palladium-Catalyzed Completely Linear-Selective Negishi Cross-Coupling of Allylzinc Halides with Aryl and Vinyl Halides.” Angew. Chem. Int. Ed. 2013, 52, 14098-14102.

407. Lee, H.G.; Milner, P.J. and Buchwald, S.L. “An Improved Catalyst System for the Pd-Catalyzed Fluorination of (Hetero)Aryl Triflates.” Org. Lett. 2013, 15. 5602-5605.

406. Zhu, S.; Niljianskul, N. and Buchwald, S.L. “Enantio- and Regioselective CuH-Catalyzed Hydroamination of Alkenes.” J. Am. Chem. Soc. 2013, 135, 15746-15749.

405. Zhu, R. and Buchwald, S.L. “Enantioselective Functionalization of Radical Intermediates in Redox Catalysis: Copper-Catalyzed Asymmetric Oxytrifluoromethylation of Alkenes.” Angew. Chem. Int. Ed. 2013, 52, 12655-12658.

404. Chen, M. and Buchwald, S.L. “Rapid and Efficient Trifluoromethylation of Aromatic andHeteroaromatic Compounds Using Potassium Trifluoroacetate Enabledby a Flow System.” Angew. Chem. Int. Ed. 2013, 52, 11628-11631.

403. Jui, N.T. and Buchwald, S.L. “Cascade Palladium Catalysis: A Predictable and Selectable Regiocontrolled Synthesis of N-Arylbenzimidazoles.” Angew. Chem. Int. Ed. 2013, 52, 11624-11627.

402. Senecal, T.D.; Shu, W. and Buchwald, S.L. “A General, Practical Palladium-Catalyzed Cyanation of (Hetero)Aryl Chlorides and Bromides.” Angew. Chem. Int. Ed. 2013, 52, 10035-10039.

401. Düfert, M.A.; Billingsley, K.L. and Buchwald, S.L. “Suzuki-Miyaura Cross-Coupling of Unprotected, Nitrogen-Rich Heterocycles: Substrate Scope and Mechanistic Investigation.” J. Am. Chem. Soc. 2013, 135, 12877-12885.

400. Cheung, C. W. and Buchwald, S.L. “Mild and General Palladium-Catalyzed Synthesis of Methyl Aryl Ethers Enabled by the Use of a Palladacycle Precatalyst.” Org. Lett. 2013, 15, 3998-4001.

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