Preparation process of trimebutine alkali

Abstract

The invention relates to the field of medicine preparation, and discloses a preparation process of trimebutine base, which comprises the following steps: taking 2-amino-2-phenylbutyric acid as a raw material, reducing the 2-amino-2-phenylbutyric acid into 2- (dimethylamino) -2-phenylbutynol, synthesizing trimebutine from the 2- (dimethylamino) -2-phenylbutynol and 3, 4, 5-trimethoxybenzoic acid in an organic solvent by using protonic acid as a catalyst, carrying out esterification and nitrogen methylation of the 2-amino-2-phenylbutyric acid simultaneously to obtain 2- (dimethylamino) -phenylbutyric acid methyl ester, and reducing by using sodium borohydride to obtain the 2- (dimethylamino) -2-phenylbutynol. When the preparation process is used for preparing THE trimebutine alkali, the reacted 2-amino-2-phenylbutyric acid is washed with water and extracted and distilled, so that the efficiency of reducing the 2-amino-2-phenylbutyric acid into the 2- (dimethylamino) -2-phenylbutyric acid is improved, toluene and liquid alkali are added to neutralize the 2- (dimethylamino) -2-phenylbutyric acid, the reaction speed is improved, the using amount of 3, 4, 5-trimethoxybenzoic acid is reduced, and the reaction cost is reduced.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation process of trimebutine base. Background technique [0002] Trimebutine base is a pharmaceutical raw material, used for gastrointestinal symptoms (such as abdominal distension, abdominal pain and gas) and irritable bowel syndrome caused by gastritis, as a drug for regulating gastrointestinal motility, due to adverse reactions The rate is only about 4.3%, and it disappears naturally after continuing to take it, and there is no case of forced drug withdrawal. It has achieved relatively great success in clinical treatment. This is one of the main gastrointestinal drugs on the market. [0003] In the process of preparation of existing trimebutine base, the efficiency of 2-amino-2-phenylbutyric acid reduction into 2-(dimethylamino)-2-phenylbutanol is relatively low, and 2-(di Methylamino)-2-phenylbutanol and 3,4, the speed of reaction of 5-trimethoxybenzoic acid is sl...

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies of the prior art, the present invention provides a preparation process of trimebutine base, which has the advantages of high reduction quality, fast reaction speed, and low preparation cost, and solves the problem of the reduction quality of trimebutine base currently on the market. Lower, slower reaction speed, and higher preparation costs