The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor

Abstract

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.

Graphical Abstract

KEYWORDS:

• AT13387
• cost-effective synthetic route
• Hsp90
• iso-indoline
• proteostasis

Additional information

Funding

The authors gratefully acknowledge the Ara Parseghian Medical Research Fund, the National Institutes of Health [CA167079], and National Cancer Institute for support.