Chemical synthesis method for epinastine

Abstract

The invention discloses a new chemical synthesizing method of yipisidin, which comprises the following steps: ammonifying 6-chloromethyl-11-dihyrogen-dibenz [b,e] aza to generate 6-aminomethyl-11-dihydrogen-dibenz [b,e] aza; reducing the 6-aminomethyl-11-dihydrogen-dibenz [b,e] aza into 6-aminomethyl-6,11-dihydrogen-5H-dibenz [b,e] aza; generating the product through cyanogen bromide to loop. Theinvention simplifies the making method with little by-product, which improves the receiving rate by 69% with high purity (HPLC. 99. 0%) for industrial manufacturing.

Description

technical field The invention relates to a novel chemical synthesis method of epinastine. It specifically relates to a method for synthesizing epinastine by using 6-chloromethyl-11-dihydro-dibenzo[b,e]azepine as a starting material through ammoniation reaction, reduction reaction and ring closure reaction . Starting material 6-chloromethyl-11-dihydro-dibenzo [b, e] azepine can be according to J.Am.Chem.Soc. Magazine 1970, Vol.13, P35 published literature method prepared. Background technique Epinastine is suitable for skin allergic reactions and has good curative effect on allergic rhinitis and allergic bronchial asthma. Wide range of clinical application departments. It has high selectivity and affinity for H1 receptors, and its anti-allergic effect is stronger than that of traditional drugs. With multiple anti-allergic mechanisms, it can eliminate allergic symptoms more thoroughly. The onset of effect is more rapid, and the pain of patients can be relieved quickly. ...

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Problems solved by technology

This line uses cyanide and precious lithium tetrahydrogen for reduction, which is not suitable for industrial production

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