Emitefur, BOF-A2, Last-F
乙嘧替氟Chemical Name: 3-[3-(6-Benzoyloxy-3-cyano-2-pyridyloxycarbonyl)benzoyl]-1-(ethoxymethyl)-5-fluorouracil
CAS No. 110690-43-2
项目整合开发状态: Phase III
项目研究机构: Otsuka (Originator)
合成路线:By condensation of 3-[3-(chlorocarbonyl)benzoyl]-1-(ethoxymethyl)-5-fluorouracil (I) with 6-benzoyloxy-3-cyano-2-hydroxypyridine (II) by means of triethylamine in refluxing acetonitrile.The starting compounds (I) and (II) are obtained as follows:The reaction of 1-(ethoxymethyl)-5-fluorouracil (III) with isophthaloyl dichloride (IV) by means of triethylamine in refluxing dioxane gives uracil (I).The esterification of 3-cyano-2,6-dihydroxypyridine (V) with benzoyl chloride (VI) by means of triethylamine in dimethylacetamide affords pyridine (II).
📌 参考资料/链接：
参考文献标题:5-Fluorouracil derivs.,process for their preparation and their use
文献作者:Fujii,S.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:DE 3709699; FR 2605006; GB 2192880; JP 1988201127; JP 1988301880
📄 详细内容
合成路线:By condensation of 3-[3-(chlorocarbonyl)benzoyl]-1-(ethoxymethyl)-5-fluorouracil (I) with 6-benzoyloxy-3-cyano-2-hydroxypyridine (II) by means of triethylamine in refluxing acetonitrile.The starting compounds (I) and (II) are obtained as follows:The reaction of 1-(ethoxymethyl)-5-fluorouracil (III) with isophthaloyl dichloride (IV) by means of triethylamine in refluxing dioxane gives uracil (I).The esterification of 3-cyano-2,6-dihydroxypyridine (V) with benzoyl chloride (VI) by means of triethylamine in dimethylacetamide affords pyridine (II).
参考文献标题:Emitefur
文献作者:Castar,J.; Hoshi,A.
参考来源:Drugs Fut 1993,18(5),418
产品链接: CAS No. 110690-43-2››