Preparation method of 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine

The invention relates to a method for preparing 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine, which is an important intermediate for preparing arginine vasopressin V2 receptor antagonist Tolvaptan. The preparation method comprises the following steps: with methyl 2-amido-5-chlorobenzoate and e...

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Bibliographic Details
Main Authors XIE XIAOSHUAI, WANG PINGBAO, LIU DENGKE, LIU YING, NIU DUAN, MU SHUAI, ZHANG DASHUAI
Format Patent
LanguageChinese
English
Published 03.04.2013
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention relates to a method for preparing 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine, which is an important intermediate for preparing arginine vasopressin V2 receptor antagonist Tolvaptan. The preparation method comprises the following steps: with methyl 2-amido-5-chlorobenzoate and ethyl 4-bromobutyrate as starting raw materials, reacting under the effect of an acid binding agent to generate secondary amine, and then carrying out Dieckman condensation and hydrolysis reaction to obtain the target compound 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. Compared with the existing method, the method provided by the invention has the advantages that the reaction steps are reduced, the operation is easy and simple, the product purity is high, and the yield is also greatly improved, thus the production cost can be reduced and the benefits are increased.
Bibliography:Application Number: CN20121483989