Synthesis method of 1,3-benzodiazepine compounds and antitumor activity

A technology for benzodiazepines and a synthesis method, which is applied in the directions of organic chemistry, drug combination, antitumor drugs, etc., can solve the problems of single product structure, difficult to obtain raw materials, low atom economy and the like, and achieves simple synthesis process and raw materials. Inexpensive and readily available raw materials
CN112174901AActive Publication Date: 2021-01-05HENAN NORMAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HENAN NORMAL UNIV
Publication Date
2021-01-05

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Abstract

The invention discloses 1,3-benzodiazepine compounds with anticancer activity and a synthesis method thereof, and belongs to the technical field of drug development. The structural general formula ofthe 1,3-benzodiazepine compounds is shown in the specification; and the synthesis method comprises the following steps: mixing N-aryl amidine 1, propargyl alcohol ester compounds 2, a rhodium or ruthenium catalyst, an additive and an organic solvent, and performing heating and reacting to obtain the 1, 3-benzodiazepine compounds 3. The synthesis method disclosed by the invention has the advantagesof simple and easily available raw materials, simplicity and convenience in operation, mild conditions, wide substrate application range and the like, and the compounds have remarkable inhibitory activity on cancer cells such as HeLa or Ramos and are potential candidate drug molecular structures.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis and drug discovery, and specifically relates to a synthesis method and anticancer activity of 1,3-benzodiazepine compounds. Background technique

[0002] As we all know, a variety of 1,3-benzodiazepines have significant anticancer, analgesic and antidepressant drug activities, and have been widely used in clinical practice, making important contributions to ensuring life and health and improving quality of life , but the existing 1,3-benzodiazepine activity studies are actually clinically applied, and there are not many drugs that have been successfully marketed.

[0003] Therefore, research and develop anti-cancer drug candidates of new 1,3-benzodiazepine compounds, find better activity than existing drugs, and then carry out structural modification, so as to screen out more potential drug molecular structures Still very much to look forward to.

[0004] At the same time, some reliabl...

Claims

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