Method for preparing secnidazole

Abstract

This invention relates to secnidazole [1-(2-hydroxy group propyl)-2-methyl-5- nitro imidazole] preparation method, it belongs to chemical pharmacy technique field. 2-methyl-5-nitro imidazole and 1-chlorine-2-propyl alcohol are materials, dry acid gas is let in to dissolve solid, then heated, distilled and recover 1-chlorine-2- propanol, pH is adjusted by sig water and cooled to 0 degree centigrade. Then it is filtrated, unreacted 2-methyl-5-nitro imidazole is recovered, filtrate pH value is adjusted to alkality, and then secnidazole crude is got after filtration. Reaction temperature is 85-95 degrees cenrigrade, reaction time is 6.0-7.5 hours, mol ratio of 2-methyl-5-nitro imidazole and 1-chlorine-2-propyl alcohol is 1:3.25-5.30. Compering to existing technique, the reaction preoceudre is only one step, generating period is shortened, and operation is simplified. Reaction whole yield is improved from less than 50 percent reported from document to 56-60 percent, and material mass using is reduced, so generating cost is reduced, generating safty is also improved.

Description

technical field

[0001] The invention relates to a preparation method of secnidazole [1-(2-hydroxypropyl)-2-methyl-5-nitroimidazole], belonging to the technical field of chemical pharmacy. Background technique

[0002] Secnidazole has a structure as shown in general formula I, and is a highly effective anti-amoeba and anti-trichomonad drug of the 5-nitroimidazole class. It is clinically used to treat various acute and chronic hepatic and intestinal amoebiasis and trichomoniasis such as urethra, female vagina, and male prostate. It is also used for the treatment of giardiasis and anaerobic infection in various parts of the human body.

[0003]

[0004] Formula I

[0005] About the preparation method of secnidazole, current bibliographical information roughly has following several kinds:

[0006] 1. Rhone-poulec S.A reported (French patent 1427627 and French patent M3270) that 2-methyl-5-nitroimidazole (1mol) was dissolved in 85% formic acid (7.88 parts), cooled to -14°C, ...

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