A novel and simple asymmetric synthesis of CMI-977 (LDP-977): a potent anti-asthmatic drug lead

被引:28
作者
Gurjar, MK [1 ]
Murugaiah, AMS
Radhakrishna, P
Ramana, CV
Chorghade, MS
机构
[1] Natl Chem Lab, Pune 411008, Maharashtra, India
[2] Chorghade Enterprise, Natick, MA 01760 USA
关键词
D O I
10.1016/S0957-4166(03)00157-5
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
A practical gram scale asymmetric synthesis of CMI-977 is described. A tandem double elimination of an a-chlorooxirane and concomitant intramolecular nucleophilic substitution was used as the key step. Jacobsen hydrolytic kinetic resolution and Sharpless asymmetric epoxidation protocols were applied for the execution of the synthesis of the key chiral building block. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1363 / 1370
页数:8
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