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

页码：1436 / 1443

页数：8

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