KCA-098
[3-(二甲基氨基甲酰氧基)-6-氧代-5H-[1]苯并呋喃并[3,2-c]喹啉-9-基]N,N-二甲基氨基甲酸酯Chemical Name: 3,9-Bis(N,N-dimethylcarbamoyloxy)benzofuro[3,2-c]quinolin-6(5H)-one
CAS No. 129794-24-7
项目整合开发状态: Preclinical
项目研究机构: Kissei (Originator)
合成路线:The cyclization of m-anisidine (I) with 2,4-dimethoxyphenylmalonic acid diethyl ester (II) in refluxing diphenyl ether (270-90 C) gives 3-(2,4-dimethoxyphenyl)-4-hydroxy-7-methoxyquinolin-2-(1H)-one (III),which is submitted to a new cyclization process in refluxing 47% aqueous HBr yielding 3,9-dihydroxybenzofuro[3,2-c]quinolin-6-(5H)-one (IV).Finally,this compound is esterified with N,N-dimethylcarbamoyl chloride (V) by means of triethylamine and dimethylaminopyridine (DMAP) in DMF.
📌 参考资料/链接：
参考文献标题:Benzofuro[3,2-c]quinoline cpds
文献作者:Kamijo,T.; Ujiie,A.; Harada,H.; Tsutsumi,N.; Tsubaki,A.; Yamaguchi,T.; Nagata,H.(Kissei Pharmaceutical Co.,Ltd.)
参考来源:AU 8930977; EP 0357172; JP 1990062878; US 5023261
📄 详细内容
合成路线:The cyclization of m-anisidine (I) with 2,4-dimethoxyphenylmalonic acid diethyl ester (II) in refluxing diphenyl ether (270-90 C) gives 3-(2,4-dimethoxyphenyl)-4-hydroxy-7-methoxyquinolin-2-(1H)-one (III),which is submitted to a new cyclization process in refluxing 47% aqueous HBr yielding 3,9-dihydroxybenzofuro[3,2-c]quinolin-6-(5H)-one (IV).Finally,this compound is esterified with N,N-dimethylcarbamoyl chloride (V) by means of triethylamine and dimethylaminopyridine (DMAP) in DMF.
参考文献标题:KCA-098
文献作者:Rabasseda,X.; Castar,J.; Mealy,N.
参考来源:Drugs Fut 1995,20(3),235
产品链接: CAS No. 129794-24-7››