The preparation method of benzodiazepine compound

A technology for benzodiazepines and compounds, which is applied in the field of preparation of benzodiazepine compounds, can solve the problems of destroying isonitrile components, complicated reaction steps, etc., and achieves the advantages of low synthesis cost, shortened reaction steps, and simple and efficient synthesis method. Effect
CN102190631BInactive Publication Date: 2014-10-29中国人民解放军63975部队
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
中国人民解放军63975部队
Publication Date
2014-10-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method of a benzodiazepine compound, which comprises the following steps: reacting amino functionalized ionic liquid, phenylpropyl aldehyde, Boc-anthranilic acid and cyclohexyl isonitrile to obtain an ionic-liquid-loaded Ugi product; reacting the ionic-liquid-loaded Ugi product under the catalytic action of hydrogen chloride gas to obtain a benzodiazepine compound of which the side chain is modified by Ugi reaction; and carrying out rotary evaporation on the reaction liquid, and washing out residues with anhydrous aether to obtain the required benzodiazepine compound. Compared with the existing preparation method, the preparation method provided by the invention shortens the reaction procedures and enhances the reaction efficiency; and the synthesis method is simple and efficient, and has wide application prospects.
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Description

technical field

[0001] The invention relates to a preparation method of a benzodiazepine compound, in particular to a benzodiazepine compound whose side chain is modified by a Ugi product through the reaction of ionic liquid loading Ugi. Background technique

[0002] Benzodiazepines are a class of compounds with a wide range of biological activities. At present, such compounds are usually synthesized by Ugi reaction, which can not only shorten the synthetic route, improve the reaction efficiency, but also play the role of side chain modification. In 1996, Thomas et al directly synthesized benzodiazepines through Ugi reaction (J.Org.Chem., 1996, 61, 8935-8939). Conventional synthetic benzodiazepines method reaction formula is as follows:

[0003]

[0004] But this multi-component (four components) condensation reaction, in the case of no load, other components in the reaction system are difficult to remove, and finally can only be purified by the method of silica gel col...

Claims

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