贝诺酯的合成

Synthesis of Benoyilate

目的:探索贝诺酯具有工业生产价值新的合成路线。方法:本合成法以扑热息痛、阿司匹林为原料,阿司匹林经氯化,扑热息痛成钠盐,二者以PEG6000为相转移催化剂酯化而得贝诺酯。结果:总收率为92%,产品质量符合《中国药典》(2000年版)标准。结论:该路线使用PEG为相转移催化剂,大大提高了收率,降低成本,具有工业生产价值。

Objective： To explore the new synthetic routh of Benorilate, which is of the value in the industrial production. Methods： Paracetamol and Aspirin was used as the raw material, Aspirin was chloridated by thiony chloride, paracetamot was neutralized by sodium hydroxide. Benorilate was produced by the reaction of o - acetoxy benzogl chloride with sodium pacetamido phenylate in the presence of PEG6000 phase transfer catalyst. Results： The total yield was 92%, and the quality of the products was according with ChP2000. Conclusion： This route is of high yield and low cost because of PEG phase transfer catalyst, so it is of the value in the industrial production.