Synthesis 2020; 52(22): 3415-3419
DOI: 10.1055/s-0040-1707346
special topic
© Georg Thieme Verlag Stuttgart · New York

Copper-Catalyzed Asymmetric Hydroamination of Styrenes with piv ZPhos as Ligand

Chengsheng Chen
,
Ling Wu
,
Yuwen Wang
,
Linglin Wu
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road/P.O. Box 368, Ridgefield, CT 06877-0368, USA   Email: yongda.zhang@boehringer-ingelheim.com   Email: linglin.wu@boehringer-ingelheim.com
,
Yongda Zhang
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road/P.O. Box 368, Ridgefield, CT 06877-0368, USA   Email: yongda.zhang@boehringer-ingelheim.com   Email: linglin.wu@boehringer-ingelheim.com
› Author Affiliations
We thank Boehringer Ingelheim Pharmaceuticals for financial support.
Further Information

Publication History

Received: 15 May 2020

Accepted after revision: 19 June 2020

Publication Date:
06 August 2020 (online)


Published as part of the Special Topic Synthesis in Industry

Abstract

A copper-catalyzed hydroamination of styrenes using piv ZPhos as ligand is reported. Enantioselectivities up to 94% are achieved under optimized conditions with aryl and heteroaryl styrenes. A variety of electrophilic O-benzoylhydroxylamines are well tolerated.

Supporting Information