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Synfacts 2017; 13(11): 1111
DOI: 10.1055/s-0036-1591403
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Commercial Synthesis of BMS-663068

Contributor(s):
Philip Kocienski
Yan M. Baran PS. * The Scripps Research Institute, La Jolla, USA
BMS-663068: Another Quiet Victory for Chemistry.

Org. Process Res. Dev. 2017;
21: 1091-1094
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Publication History

Publication Date:
19 October 2017 (online)

 
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Key words

BMS-663068 - HIV attachment inhibitor - scalable synthesis

Significance

The entire issue 8 of Organic Process Research & Development is devoted to an extraordinarily detailed account of the development of a commercial synthesis of the HIV attachment inhibitor BMS-663068 by workers at Bristol-Myers Squibb. The strategy, tactics and mechanistic illumination that transformed enabling routes to a commercial process that delivered >1000 kg of API are presented in nine back-to-back papers.


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Comment

By way of an overture, Yan and Baran provide a graphical synopsis of the synthesis (see Scheme), innovations and key achievements. Every atom of BMS-663068 is derived from economical, readily available, safe, and easily handled compounds, thereby ensuring a robust and secure supply chain for all raw materials. Moreover, the synthesis is noteworthy for being free of challenging reaction conditions.


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