Preparation method of alprazolam intermediate

A technology of alprazolam and intermediates, which is applied in the field of preparation of alprazolam intermediates and achieves the effects of shortening reaction time, short reaction time and environmental friendliness
CN108250091AInactive Publication Date: 2018-07-06山东安信制药有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
山东安信制药有限公司
Publication Date
2018-07-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of an alprazolam intermediate. The method comprises the following steps: sequentially adding methanol and p-nitrochlorobenzene in a sodium hydroxide watersolution, dropwise adding phenylacetonitrile under stirring, reacting at 40 + / -5 DEG C after the dropwise addition is finished, and carrying out post-treatment to obtain an intermediate (II) ; and dissolving the intermediate (II) in ethanol, adding iron powder, refluxing, dropwise adding sulfuric acid, refluxing for 1 hour, and carrying out post-treatment to obtain an intermediate(III). Accordingto the method disclosed by the invention, the sodium hydroxide water solution is used in the synthesis of the intermediate (II) to replace a dangerous mode of refluxing and dissolving solid sodium hydroxide by using ethanol, a small amount of methanol is added into the reaction system, and the problem of two-phase reaction is successfully solved. The sulfuric acid is used for replacing volatile hydrochloric acid during the synthesis of the intermediate (III), the reaction time is effectively shortened, and the reaction efficiency is improved. The method disclosed by the invention is safer to operate, short in reaction time and more suitable for industrial production.
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Description

technical field

[0001] The invention relates to the technical field of drug synthesis, in particular to a preparation method of an alprazolam intermediate (2-amino-5-chlorobenzophenone). Background technique

[0002] Alprazolam, chemical name: 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3,α]benzodiazepine , the structural formula is as follows. Alprazolam is a central system depressant developed in recent years, commonly used in the treatment of insomnia, anxiety, depression and other psychoneurological symptoms. The alprazolam molecule contains a metabolically stable triazole ring, so its physiological activity is stronger than that of general benzodiazepines, its sedative effect is 25-30 times that of diazepam, and its hypnotic effect is 3.5-3 times that of diazepam. 11.3 times, and it also has obvious anti-epileptic and anti-depressant effects.

[0003]

[0004] At present, many preparation methods about alprazolam have been reported. Method 1: Synthesize a dia...

Claims

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