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Updated: Sep 28, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Development of an atropselective methodology for axially chiral biaryls in the asymmetric synthesis of A-240610.0
1Abbott Laboratories, GPRD Process Research, D-R450, Building R-13, 1401 Sheridan Road, North Chicago, IL 60064, USA. yiyin.ku@abbott.com
Abstract:
A-240610.0 is a novel non-steroidal glucocorticoid receptor-selective ligand. It has demonstrated an anti-inflammatory activity equivalent to that of the synthetic glucocorticoids, and has shown an improved side-effects profile in vivo. This review will present the process research and development proceeding from the initial racemic route to an efficient asymmetric process. This process relied on the development of a novel atropselective synthesis of an axially chiral biaryl to form the critical atropisomer intermediate in good yields (85%) and with high diastereoselectivity (99:1).
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