Synthesis of the major metabolites of Tolvaptan

作     者：Wei Li Wan Jian Bo Wu Fan Lei Xiao Long Li Li Hai Yong Wu 

作者机构：Key Laboratory of Drug Targeting and Drug Delivery System of the Education MinistryDepartment of Medicinal ChemistryWest China School of PharmacySichuan University 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2012年第23卷第12期

页      面：1343-1346页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：financial support from the Sichuan Baili Pharmaceutical Co. Ltd 

主　　题：Tolvaptan Metabolites Synthesis 

摘      要：Tolvaptan is a nonpeptide arginine vasopressin （AVP） V2-receptor antagonist and used in the treatment of heart failure, cirrhosis, syndrome of inappropriate antidiuretic hormone secretion or other high-volume capacity of hyponatremia. The metabolites of tolvaptan are mainly produced by CYP3A4, including two major compounds named DM-4103 and DM-4107. Herein, the chemical synthesis of those two metabolites is described in this article for further study.