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

• Main Authors: XIE XIAOSHUAI, WANG PINGBAO, LIU DENGKE, LIU YING, NIU DUAN, MU SHUAI, ZHANG DASHUAI
• Format: Patent
• Language: Chinese; English
• Published: 03.04.2013
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

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.