Synthesis of Tolvaptan
pick up all this at
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)
(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%.
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%.
【Key Words】： tolvaptan arginine vasopressin V_2 receptor antagonist heart failure hyponatremia synthesis
【Fund】： 天津市科技计划项目(09ZCKFSH01300)
【CateGory Index】： R914
【Fund】： 天津市科技计划项目(09ZCKFSH01300)
【CateGory Index】： R914
CAJViewer7.0 supports all the CNKI file formats; AdobeReader only supports the PDF format.
| 【Citations】 | ||
| |||||
| |||||
| 【Co-citations】 | ||
| |||
| |||
No comments:
Post a Comment