1-OXOISOQUINOLINE AND PRODUCTION THEREOF

摘要

PROBLEM TO BE SOLVED: To obtain the subject novel 1-oxoisoquinolines that has aldose reductase inhibitory activity and is effective for treatment of a variety of diabetic complications with cataract, retinopathy, neuropathy, nephropathy or the like. SOLUTION: This compound is represented by formula I R1-R3 are each H, a (substituted) 1-20C alkyl, a (substituted) 1-4C alkylaryl or a (substituted) aryl; R4 is H or the formula: CH2CO2R5 [R5 is H, a (substituted) 1-20C alkyl, a (substituted) 1-4C alkylaryl or the like]}, typically the compound of formula II. The compound of formula I is prepared, for example, by converting any of R1-R3 is converted to H, when necessary, or either R1 or R2 is used as a suitable protecting group for hydroxyl groups in an isocoumarin derivative and aminating the isocoumarin with ammonia or primary amines to convert to the corresponding isoquinoline derivative.