发明名称 WATER-SOLUBLE CAMPTOTHECIN DERIVATIVE
摘要 PROBLEM TO BE SOLVED: To obtain a new compound useful as an intermediate for producing a water-soluble camptothecin derivative used for treating tumors. SOLUTION: A compound of formula I [(n) is 1 or 2; R1, R2 are each H, a 1-6C alkyl or the like, or R1 is H, a 1-6C alkyl or the like and R2 is a group of the formula; COR3, or R1 and R2 are bonded to each other together with a nitrogen atom bonded thereto to form a saturated three to seven-membered heterogeneous group; R3 is H, a 1-6C alkyl or the like; Y is O, S or the like], for example, 2'-amino-4',5'-methylenedioxy-2-trifluoroacetamidoacetophenone. The compound of formula I is obtained by reacting a compound of formula III (X is a halogen) (for example, 2'-amino-4',5'-methylenedioxy-2- chloroacetophenone) with a compound of the formula: HNR1R2 (for example, trifluoroacetamine) in the presence of a base in an aprotic polar solvent such as acetonitrile.
申请公布号 JP2000109475(A) 申请公布日期 2000.04.18
申请号 JP19990312940 申请日期 1999.11.02
申请人 GLAXO INC 发明人 LUZZIO MICHAEL J;BESTERMAN JEFFREY M;EVANS MICHAEL G;MYERS PETER LESLIE
分类号 A61K31/47;A61K31/435;A61K31/4738;A61K31/4745;A61K31/496;A61K31/5377;A61K31/541;A61P35/00;A61P43/00;C07D317/66;C07D319/18;C07D491/22;C07D498/22;(IPC1-7):C07D317/66 主分类号 A61K31/47
代理机构 代理人
主权项
地址