Benzodiazepinic amine nitrite compound, preparation and use thereof

Abstract

The invention relates to a 1, 4-nitrosation-N-nitrosamine intermediate (I) compound in the synthesis of alprazolam, a preparation method and application thereof to the preparation of alprazolam. 7-chloro-5-phenylbenzodiazepinone is taken as an initial raw material, and the alprazolam is obtained by the synthesis through certain processes such as condensation ring-closure after a methylamination reaction and an N-nitrosation reaction. Other benzodiazepine derivatives can be synthesized through a 1, 4-nitrosation-N-nitrosamine intermediate obtained by the synthesis. The method has the advantages of unique process, steady product quality, mild process conditions, easy control, and high yield, and can control lower production cost and reduce environmental pollution.

Description

technical field [0001] The invention relates to a kind of 1,4-benzodiazepine in the synthesis of alprazolam —N-nitrosamine intermediate compound and its preparation method and its application in the preparation of alprazolam belong to the field of chemical technology. Background technique [0002] Benzodiazepine Benzodiazepines are heterocyclic compounds with a wide range of physiological activities and pharmacological effects. These compounds have sedative, anticonvulsant, anticonvulsant, hypnotic, anxiolytic and antidepressant effects. Some of these compounds are widely used clinically as hypnotic tranquilizers. Studies in recent years have found that some of these heterocyclic compounds have anti-AIDS activity. Alprazolam is a third-generation central nervous system depressant drug developed in recent years. It was launched in the United States in 1981 and is commonly used to treat psychoneurological symptoms such as insomnia, anxiety, and depression. Because its mo...

AI Technical Summary

Problems solved by technology

Belupo et al. used triethyl orthoformate instead of acetylhydrazide for cyclization in HR P20010081. The condensation ring closure reaction needs to be carried out under absolutely anhydrous conditions, and the reaction conditions are harsh, which is not conducive to industrial-scale production

Although the condensation ring-closing reaction is different, the above two routes need to carry out vulcanization catalytic reaction, which uses high-flammability and dangerous substances, which has caused serious pollution to the environment.

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