罗氟司特新合成工艺的研究  

Studies on Process of Synthesizing Roflumilast

作　　者：曹一帆[1] 刘昭文[2] 郭小华[2] 杨凯[2] 

机构地区：[1]南昌大学化学学院,南昌330031 [2]赣南医学院药学院,赣州341000

出　　处：《海峡药学》2016年第3期231-232,共2页Strait Pharmaceutical Journal

摘　　要：目的优化罗氟司特的合成工艺。方法以3,4-二羟基苯甲醛为起始原料,经Boc酸酐保护、醚化、脱保护、二氟一氯甲烷醚化、氧化、酰胺化反应得到目标物罗氟司特。结果与结论目标化合物的结构经MS、1H-NMR等确证。该方法原料易得,反应条件温和,危险性小,后处理简单,收率较高,有利于工业放大生产,总收率为36.3%。OBJECTIVE To optimize the synthetic procedure of Roflumilast. METHODS Roflumilast was synthesized from 3,4-dihydroxybenzaldehyde by the reactions of Boc anhydrides protection,etherification,deprotection,monochlorodifluoromethane etherification,oxidation,amidation. RESULTS and CONCLUSION The structure of roflumilast was confirmed by MS and 1H-NMR. The synthesized route was rewarded for virtue of easy access of materials,kindness of reaction conditions,low dangerness,easy reprocessing,and good yield of 36. 3%,which are the advantages for industry.

关 键 词：3 4-二羟基苯甲醛 醚化 罗氟司特 

分 类 号：R91[医药卫生—药学]