Synlett 2019; 30(14): 1693-1697
DOI: 10.1055/s-0037-1610722
cluster
© Georg Thieme Verlag Stuttgart · New York

Rhodium-Catalyzed Asymmetric Addition of Arylboronic Acids to Glyoxylates: Access to Optically Active Substituted Mandelic Acid Esters

Diao Chen
a   State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, P. R. of China
,
Jian-Guo Liu
b   Shenzhen Grubbs Institute and Department of Chemistry, Southern University of Science and Technology, 1088 Xueyuan Blvd., Shenzhen 518055, P. R. of China   Email: xumh@sustech.edu.cn
,
Xu Zhang
a   State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, P. R. of China
,
Ming-Hua Xu
a   State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, P. R. of China
b   Shenzhen Grubbs Institute and Department of Chemistry, Southern University of Science and Technology, 1088 Xueyuan Blvd., Shenzhen 518055, P. R. of China   Email: xumh@sustech.edu.cn
› Author Affiliations
The National Science & Technology Major Project (2018ZX09711002-006), National Natural Science Foundation of China (81521005, 21472205, 21325209)
Further Information

Publication History

Received: 31 May 2019

Accepted after revision: 25 June 2019

Publication Date:
17 July 2019 (online)


D.C. and J.G.L. contributed equally.Published as part of the Cluster Organosulfur and Organoselenium Compounds in Catalysis

Abstract

A rhodium-catalyzed enantioselective addition of glyoxylates to arylboronic acids promoted by a simple chiral sulfinamide-based olefin ligand under mild reaction conditions is described. The reaction provides access to a variety of optically active substituted mandelic acid esters in good yields with up to 83% ee. The catalytic system is also applicable to pyruvate addition. The synthetic utility of this method is highlighted by a formal synthesis of the antiplatelet drug clopidogrel.

Supporting Information