文献类型：期刊文献

英文题名：Highly Enantioselective Rhodium-Catalyzed Addition of Arylboroxines to Simple Aryl Ketones: Efficient Synthesis of Escitalopram

作者：Huang, Linwei[1];Zhu, Jinbin[1];Jiao, Guangjun[2];Wang, Zheng[3];Yu, Xingxin[1];Deng, Wei-Ping[1];Tang, Wenjun[1,2]

机构：[1]E China Inst Theoret Phys, Shanghai Key Lab New Drug Design, Sch Pharm, 130 Mei Long Rd, Shanghai 200237, Peoples R China;[2]Chinese Acad Sci, State Key Lab Bioorgan & Nat Prod Chem, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China;[3]AstraZeneca Global R&D, Innovat Ctr China, Beijing, Peoples R China

年份：2016

卷号：55

期号：14

起止页码：4527

外文期刊名：ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

收录：;EI(收录号：20161002066591);WOS:【SCI-EXPANDED(收录号:WOS:000373133000020)，CCR-EXPANDED(收录号:WOS:000373133000020)】；

基金：We are grateful to NSFC-21432007, 21272254, 21572246, the "Thousand Plan" Youth program.

语种：英文

外文关键词：asymmetric catalysis; enantioselectivity; ligand design; rhodium; total synthesis

摘要：Highly enantioselective additions of arylboroxines to simple aryl ketones have been achieved for the first time with a Rh/(R,R,R,R)-WingPhos catalyst, thus providing a range of chiral diaryl alkyl carbinols with excellent eevalues and yields. (R,R,R,R)-WingPhos has been proven to be crucial for the high reactivity and enantioselectivity. The method has enabled a new, concise, and enantioselective synthesis of the antidepressant drug escitalopram.