The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor

被引：1
|
作者：
Kaur, Jatinder [1 ]
Bhardwaj, Atul [1 ]
Melancon, Bruce J. [1 ]
Blagg, Brian S. J. [1 ]
机构：
[1] Univ Notre Dame, Dept Chem & Biochem, Warren Family Res Ctr Drug Discovery & Dev, Notre Dame, IN 46556 USA
来源：
SYNTHETIC COMMUNICATIONS | 2019年 / 49卷 / 11期
基金：
美国国家卫生研究院;
关键词：
AT13387; cost-effective synthetic route; Hsp90; iso-indoline; proteostasis; MOLECULAR CHAPERONES; DISCOVERY; COMPLEX;
D O I：
10.1080/00397911.2019.1602654
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
AT13387 is an orally bioavailable clinical candidate developed to inhibit heat shock protein 90 (Hsp90). This article describes a modified synthetic route for the multi-gram production of AT13387 in 46% overall yield. The modified synthetic route is short, avoids stringent reaction conditions and difficult purifications, which led to an increase in overall yield.
引用
收藏
页码：1436 / 1443
页数：8
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