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Sunday, 1 September 2013

Synthesis of Tolvaptan

Synthesis of Tolvaptan


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YANG Chuanwei~1,MU Shuai~2,LIU Ying~3,WANG Pingbao~3,LIU Dengke~(3*) 
(1.School of Pharmacy,Henan University,Kaifeng 475004;2.
School of Chemical Engineering and Technology,
 Tianjin University,Tianjin 300072;3.
Tianjin Institute of Pharmaceutical Research,Tianjin 300193)  
Tolvaptan,a selective nonpeptide arginine vasopressin V_2 receptor antagonist,was synthesized
 from 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine by acylation and reduction to give 1-(4-amino-2-methylbenzoyl) -7- chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine,which was subjected to acylation with 2-methylbenzoyl chloride and reduction with sodium borohydride with an overall yield of about 45%.
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【Citations】
Chinese Journal Full-text Database2 Hits
1LI Fan1, HOU Xingpu2, LI Lin1, LU Tao1, DU Yumin1 (1. School of Pharmacy,
Hebei Medical University, Shijiazhuang 050017; 2. Shijiazhuang
 Pharma Group NBP Pharmaceutical Co., Ltd., Shijiazhuang 052160);
Synthesis of Antiparkinsonian Agent Istradefylline[J];Chinese Journal of Pharmaceuticals;2010-04
2YANG Miao~1,SHUAI Jun~2,LIU Mo~3,LIU Deng-ke~(3*),WANG Ping-bao~3
(1.Tianjin Medical University,Tianjin 300070;2.Tianjin University;Tianjin 300072;
 3.Tianjin Institute of Pharmaceutical Research,Tianjin 300193);
Synthesis of 7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine[J];
Chinese Journal of Pharmaceuticals;2009-09
【Co-citations】
Chinese Journal Full-text Database1 Hits
1XIONG Xiao-yi,CHEN An-qun,HE Yong-mei(Chongqing Unis Chemical Co.,Ltd.,Chongqing
402161,China);Analysis of Cyanoacetic Acid Content by HPLC[J];Guangzhou Chemical Industry;2010-12

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