| 摘要 |
<p>PURPOSE:To obtain a new compound useful as an eye drops for curing glaucoma, having excellent cornea permeation, CAMP accumulation action and intraocular tension lowering action. CONSTITUTION:The compound is expressed by the formula I [R1 is a protective group eliminable in eyes, preferably a group of the formula II (R4 and R5 are H and alkyl; R6 is 1-18C aliphatic acyloxy, etc.; R7 is the same group as R6, OH, etc.; m is 0-3), R2 and /R<3> are H or a protective group of OH],e.g. griseolic acid 8',9'-(4-acetoxybenzyl) ester, etc.). A compound of the formula I can be obtained by using a compound of the formula III as a raw compound, and subjecting 2-10 equivalent esterification agent of the formula R1-X (X is a eliminable group, preferably halogen, diazo, etc., arylsulfoxy, etc.) in a solvent (preferably dimethylamide, etc.) in the presence of an acid removing agent (preferably triethylamine, etc.).</p> |
