发明名称 METHOD AND REAGENTS FOR N-ALKYLATING UREIDES
摘要 A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure (I) with an alkylating agent of structure (III) in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N'-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.
申请公布号 WO9918084(A1) 申请公布日期 1999.04.15
申请号 WO1998US20665 申请日期 1998.10.02
申请人 TARO PHARMACEUTICAL INDUSTRIES LTD.;GUTMAN, DANIELA;HERZOG, HERSHEL 发明人 GUTMAN, DANIELA;HERZOG, HERSHEL
分类号 A61K31/496;A61K31/515;A61P25/00;A61P25/08;C07C231/08;C07C233/90;C07C273/18;C07C275/48;C07D207/40;C07D207/408;C07D211/88;C07D233/74;C07D239/62;C07D263/44;(IPC1-7):C07D239/62 主分类号 A61K31/496
代理机构 代理人
主权项
地址