Method for preparing benzodiazepine compounds

A benzodiazepine and diazepine technology, which is applied in the field of preparation of benzodiazepine compounds, can solve the problems of high catalyst selectivity, high reaction temperature, large raw material damage, etc. Explosion risk, improved reaction yield, reduced hazard effects
CN103804384AActive Publication Date: 2014-05-21李宏 +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
李宏
Publication Date
2014-05-21

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Abstract

The invention relates to a method for preparing benzodiazepine compounds, and discloses a method for preparing 8-R2-6-(2-R1-phenyl)-1-methyl-3a,4-dihydro-3H-imidazo[1,5-a][1,4] benzodiazepine (midbody II) and 8-R2-6-(2-R1-phenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine (product III), wherein R is hydrogen, fluorine, chlorine, bromine or iodine; R2 is fluorine, chlorine, bromine or iodine. The midbody II is prepared from 7-R2-5-(2-R1-phenyl)-2-aminomethyl-2,3-dihydro-1H-[1,4] benzodiazepine and triethyl orthoacetate as raw materials through ultrasonic reaction; the product III is prepared by performing enzyme dehydrogenation on the midbody II. By adopting the technical scheme of the invention, the dehydrogenation reaction selectivity is improved, and the reaction yield is improved.
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Description

technical field

[0001] The invention relates to a preparation method of benzodiazepine compounds, in particular to a preparation method of 4H-imidazo[1,5-a][1,4]benzodiazepine compounds. Background technique

[0002] Benzodiazepines are heterocyclic compounds formed by condensing a benzene ring and a seven-membered nitrogen-containing heteroatom ring. The activity of neurons in the limbic system attenuates its activation of the reticular formation. At the same time, the special effect on the limbic system can effectively reduce emotional activities, and has a good effect on anxiety and insomnia, and can produce approximate physiological sleep. These drugs have a high therapeutic index, little impact on breathing, and a wide range of safety. They have almost no effect on liver drug enzymes, and do not affect the metabolism of other drugs. Among them, 1,4-benzodiazepine and 1,3-imidazole ring are cyclized to generate 4H-imidazo[1,5-a][1,4]benzodiazepine compounds, which can ...

Claims

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