降脂药苯扎贝特合成工艺改进

Improved synthesis of hypolipidemic drug bezafibrate

目的:改进降脂药苯扎贝特的合成工艺。方法:以对氯苯甲酰氯和对羟基苯乙胺为原料先合成N-对羟基苯乙基-4-氯苯甲酰胺,再在相转移催化下与丙酮、氯仿于甲苯中缩合得到苯扎贝特。结果:目标化合物经核磁共振氢谱(1H-NMR)等确证其化学结构,缩合总收率为73%。结论:该工艺不但避免了无水操作,提高了收率,而且溶剂可通过萃取与产物分离,简化了操作,更适于工业化生产。

Objective：To improve the synthesis process of hypolipidemic drug bezafibrate.Methods： Starting from 4-chlorobenzoyl chloride and tyramine,N-（4-chlorobenzoyl）-tyramine was obtained,and then condensed with acetone and chloroform in presence of PTC in toluene to synthesis bezafibrate.Results： The structure of bezafibrate was confirmed by 1H-NMR.The overall yield of condensation reaction was up to 73%.Conclusion： The improved synthetic process with higher yield and simplified operation,free from the anhydrous condition.The solvent can be isolated via extraction.Thus it is applicable to manufacture.