Novel method for synthesizing 2,3,4,5-tetrahydric--1H-1,4-benzodiazepine

Abstract

The present invention relates to a preparation method of an organic compound, in particular to a method used for synthesizing 2, 3, 4, 5-tetrahydro-1H-1, 4-benzodiazepine. The raw materials of o-halogen benzyl halogen and ethylene have mixing reaction in an organic solvent; the intermediate product of N-(2-benzyl) ethylene diamine can be prepared after separation and purification; then the intermediate product is dissolved in the system of ring-closing agents; under the condition with a catalyst, the final product can be prepared through ring-closing reaction. Compared with the synthetic method in the prior art, the preparation method of the 2, 3, 4, 5-tetrahydro-1H-1, 4-benzodiazepine has the significant advantages of simple synthetic process, wide range of technical conditions, safe andeasy operation, environmentally friendly operation, cheap and easily available raw materials, great decrease of the production cost, high yield of the final product, high purity of the product, and broader application prospects.

Description

1. Technical field: [0001] The present invention relates to a method for the preparation of organic compounds. 2. Technical background: [0002] Benzodiazepines are very important pharmaceutical intermediates and are widely used in the pharmaceutical industry. The company has developed 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine in 2007 The mature production process, and has been industrialized production, the process route is as follows: [0003] [0004] Since the first step in this process route uses the solvent pyridine, the smell is relatively strong, and the operating environment is poor. The second step of the carbonyl reduction in the reaction requires operation under anhydrous conditions, the reaction conditions are harsh, and the flammable reducing agent IV is used. Lithium aluminum hydride (LiAlH 4 ), leading to high production costs and potential safety hazards, so it is imperative to develop new and lower-cost process routes. 3. Contents of the invention: ...

AI Technical Summary

Problems solved by technology

[0004] Since the first step in this process route uses the solvent pyridine, the smell is relatively strong, and the operating environment is poor. The second step of the carbonyl reduction in the reaction requires operation under anhydrous conditions, the reaction conditions are harsh, and the flammable reducing agent IV is used. Lithium aluminum hydride (LiAlH 4 ), leading to high production costs and potential safety hazards, so it is imperative to develop new and lower-cost process routes

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