摘要
二苯乙腈与1,2-二溴乙烷经取代,与2-甲基咪唑缩合制得4-(2-甲基-1H-咪唑-1-基)-2,2-二苯基丁腈(6),6成盐酸盐后用氢氧化钾水解得咪达那新,总收率51.2%,HPLC纯度为99.5%。咪达那新在氢氧化钾水解下制得主要有关物质4-(2-甲基-1H-咪唑-1-基)-2,2-二苯基丁酸,HPLC纯度为98%。
Imidafenacin was obtained from diphenylacetonitrile via substitution with 1,2-dibromoethane, condensation with 2-methylimidazole to give 4-（2-methyl-lH-imidazol-l-yl）-2,2-diphenylbutyronitrile, which was subjected to salt formation with hydrochloric acid and hydrolysis with potassium hydroxide with the overall yield of 51.2% and the HPLC purity of 99.5 %. The main impurity 4- （2-methyl-lH-imidazol-1-yl） -2,2-diphenylbutanoic acid was synthesized from imidafenacin via hydrolysis with potassium hydroxide with the HPLC purity of 98 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第1期10-12,共3页
Chinese Journal of Pharmaceuticals
