Chinese Chemical Letters

Synthesis of the major isomers of Aprepitant and Fosaprepitant

WL Wan, Y He, M Guan, XL Li, X Cheng, Y Wu

Index: Wan, Wei-Li; He, Yun; Guan, Mei; Li, Xiao-Long; Cheng, Xu; Wu, Yong Chinese Chemical Letters, 2013 , vol. 24, # 12 p. 1118 - 1122

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Abstract

Abstract The synthesis of two isomers of Aprepitant (APT) and three isomers of Fosaprepitant (FPT), crucial components for quality control in manufacturing, is described. Herein, three chiral centers in the isomers of Aprepitant are established in high yield by induced crystallization and chiral reduction. Additionally, the isomers of Aprepitant are utilized to synthesize the isomers of Fosaprepitant with the same stereochemistry. All the ...