Production indapamide

Abstract

A process for preparing indapamine includes such steps as dissolving 4-Cl-3- sulfamino formyl chloride and 1-amino-2-methyl-indoline in tetrahydrofuran, dripping triethylamine, condensation reaction, and post-processing. It has high output rate.

Description

(1) Technical field The present invention relates to a kind of preparation method of compound indapamide, belongs to chemical industry and chemical medicine field. (2) Background technology The chemical name of indapamide is 4-chloro-3-sulfonyl-N-(2,3-dihydro-2-methyl-1H-indole) benzamide, and its structural formula is as follows: Indapamide is a new type of antihypertensive drug with diuretic effect and calcium ion antagonistic effect, and it can also work synergistically with other antihypertensive drugs. It has the advantages of good antihypertensive effect, long action time, small side effects, and long-term use. The compound patent US3565911 discloses the synthesis method of indapamide, 1-amino-2-methylindoline and triethylamine are dissolved in tetrahydrofuran, and 4-chloro-3-sulfamobenzoyl chloride is slowly added dropwise under stirring The tetrahydrofuran solution was then concentrated to dryness and crystallized from isopropanol / water to obtain indapamide wit...

AI Technical Summary

Problems solved by technology

The purpose of the present invention is to disclose a preparation method of indapamide with few side reactions, high yield and easy control, so as to solve the problem of low yield and 4-chloro-3-sulfonamide in the production process in the prior art. The tetrahydrofuran liquid volume of benzoyl chloride is larger, the dropping time is longer, and 4-chloro-3-sulfamobenzoyl chloride is prone to self-condensation reaction under the action of triethylamine, resulting in 1-amino-2-methylind Indoline is difficult to react completely, etc.