General synthesis of conformationally constrained noncanonical amino acids with C(sp3)-rich benzene bioisosteres

03 January 2024, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Recent years have seen novel modalities emerge for the treatment of human diseases resulting in an increase in beyond rule of 5 (bRo5) chemical matter. As a result, synthetic innovations aiming at enabling rapid access of complex bRo5 molecular entities become increasingly valuable for medicinal chemists’ tool-kits. Herein, we report the general synthesis of a new class of noncanonical amino acids (ncAA) with a cyclopropyl back-bone to achieve conformational constraint and bearing C(sp3)-rich benzene bioisosteres. We also demonstrate preliminary studies towards utilities of these ncAA as building blocks for medicinal chemistry research.

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