Route exploration and synthesis of the reported pyridone-based PDI inhibitor STK076545

Author:

Greve Eric1234,Lindeman Sergey V.1234,Scartelli Christina56789,Lin Lin56789,Flaumenhaft Robert56789,Dockendorff Chris1234ORCID

Affiliation:

1. Department of Chemistry

2. Marquette University

3. Milwaukee

4. USA

5. Division of Hemostasis and Thrombosis

6. Department of Medicine

7. Beth Israel Deaconess Medical Center

8. Harvard Medical School

9. Boston

Abstract

A 5-step synthesis of a reported PDI inhibitor was developed using an aldol reaction with an allyl ester. Conventional approaches for preparing β-keto amides with a pyridone in the alpha position were complicated by undesired fragmentations or rearrangements.

Funder

Foundation for Women's Wellness

Arthur J. Schmitt Foundation

Marquette University

National Heart, Lung, and Blood Institute

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

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