Synthesis of the major isomers of Aprepitant and Fosaprepitant  

作　　者：Wei-Li Wan Yun He Mei Guan Xiao-Long Li Xu Cheng Yong Wu 

机构地区：[1]Key Laboratory of Drug Targeting and Drug Delivery System of the Education Ministry,Department of Medicinal Chemistry,West China School of Pharmacy,Sichuan University [2]West China Hospital,Sichuan University

出　　处：《Chinese Chemical Letters》2013年第12期1118-1122,共5页中国化学快报（英文版）

基　　金：fnancial support from Sichuan provincial science and technology support program (No. 2011SZ0014)

摘　　要：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 target compounds were confirmed by elemental analyses, 1R, NMR and MS data analysis.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 target compounds were confirmed by elemental analyses, 1R, NMR and MS data analysis.

关 键 词：J Aprepitant and Fosaprepitant Major isomers Chemical synthesis 

分 类 号：O621.3[理学—有机化学]