摘要
以3,4-二羟基-5-硝基苯甲酸为起始物料,经苄基醚化、酯化、酯基水解得3,4-二苄氧基-5-硝基苯甲酸,再与2,5-二氯-N-羟基-4,6-二甲基烟碱偕胺肟发生缩合后关环、氧化、脱苄基制得帕金森症治疗药物奥匹卡朋,总收率27.2%,纯度达99.3%,改进后的路线原料来源方便,操作简单,具有工业化生产前景。
As a drug for the treatment of Parkinson＇s disease, Opicapone was obtained using 3,4-dihydroxyl-5- nitryl-benzoic acid as the starting material followed by etherifieation, esterification, hydrolysis, condensation reaction with 2,5-dichlorine-N-hydroxyl--4,6-dimethyl-nicotineamidoxime, cyclization, oxidation, and debenzylation. The overall yield was 27.2% with a purity of 99.3%. This synthetic process is simple and easy for industrial operation with high yield and wide raw material sources.
出处
《精细化工中间体》
CAS
2016年第2期41-43,共3页
Fine Chemical Intermediates
