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DOI: 10.1055/s-0036-1591403
Commercial Synthesis of BMS-663068
Publication History
Publication Date:
19 October 2017 (online)
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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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