Chinese Chemical Letters

… of novel bifunctional organocatalysts: Highly enantioselective alcoholysis of meso cyclic anhydrides and its application for synthesis of the key intermediate of P2X 7 …

HJ Yang, FJ Xiong, J Li, FE Chen

Index: Yang, Hong-Jun; Xiong, Fang-Jun; Li, Jie; Chen, Fen-Er Chinese Chemical Letters, 2013 , vol. 24, # 7 p. 553 - 558

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Citation Number: 7

Abstract

A family of novel squaramides/sulfamides based on 1, 2-alkamine was developed as chiral bifunctional catalysts to promote the asymmetric alcoholysis of meso cyclic anhydrides. The hemiesters were obtained in high yield with up to 93% ee. The usefulness of this methodology was demonstrated in the asymmetric synthesis of the key intermediate of P2X7 receptor antagonists.