Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character

Campbell, Peter S. and Jamieson, Craig and Simpson, Iain and Watson, Allan J. B. (2017) Practical synthesis of pharmaceutically relevant molecules enriched in sp3 character. Chemical Communications (London). ISSN 0009-241X

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    Abstract

    The expedient synthesis of compounds enriched in sp3 character is key goal in modern drug discovery. Herein, we report how a single pot Suzuki-Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields. The approach has been successfully applied in formats amenable to parallel synthesis, in an asymmetric sense, and in the preparation of molecules with annotated biological activity.