摘要
2,3,5-三甲基吡啶经氧代、硝化、在乙酐中重排、水解及氯代制得2-氯甲基-3,5-二甲基-4-硝基吡啶盐酸盐,与2-巯基-5-甲氧基苯并咪唑在甲醇钠作用下同时完成缩合、甲氧基化得到5-甲氧基-2-[(4-甲氧基-3,5-二甲基吡啶-2-基)甲硫基]-1H-苯并咪唑,最后氧化得到奥美拉唑,总收率约42%。
Omeprazole, a proton pump inhibitor, was synthesized from 2,3,5-trimethylpyridine by oxidation, nitration, rearrangement in acetic anhydride, hydrolysis and chlorination to give 2-chloromethyl-3,5- dimethyl-4-nitropyridine hydrochloride, which was subjected to condensation and methoxylation with 2-mercapto-5- methoxybenzimidazole in presence of CH3ONa followed by oxidation with an overall yield of about 42 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2007年第2期78-80,共3页
Chinese Journal of Pharmaceuticals
