ISOQUINOLINONE DERIVATIVE, ITS PRODUCTION AND 5-HT3 RECEPTOR ANTAGONIST CONTAINING THE DERIVATIVE AS ACTIVE COMPONENT

摘要

PURPOSE:To obtain the subject compound having 5-HT3 receptor antagonistic action by hydrolyzing a specific compound under acidic condition. CONSTITUTION:The objective derivative of formula II [R1 is H, halogen, NR4R5 (R4 is H, 1-4C alkyl, etc.), etc.] or its non-toxic acid addition salt is produced by hydrolyzing a compound of formula I [R2 is H or 1-4C alkyl; R3 is H or 1-4C alkyl; R10 is triphenylmethyl, trimethylsilyl, etc. ; R11 is H, halogen or NR41R5 (R41 is 1-4C alkyl or 2-4C alkanoyl; R5 is H, 1-4C alkyl, etc.); the bond expressed by solid line and dotted line is single bond or double bond] in water and/or an organic solvent miscible with water (e.g. methanol) using an aqueous solution of an organic acid (e.g. acetic acid) at 0-90 deg.C. The compound of formula II is e.g. 2-(5-methylimidazolyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinolin-1-one.