摘要 |
<p>PURPOSE:To provide a new, low toxic compound having aldose reductase- inhibitory activity, useful for therapeutic agents for diabetic complications such as cataract, nerve disorder and nephropathy. CONSTITUTION:The objective compound of formula I (R<1> and R<2> are each H, halogen, trifluoromethyl, lower alkyl, lower alkoxy or nitro; R<3> is H, halogen or lower alkyl), e.g. 2-(4-bromo-2-fluorobenzyl)-[1,2,3,4-tetrahydropyrrolo[1,2- a]pyrazine-4-spiro-3'-pyrrolidine]1,2',3,5'-tetraone. The compound of the formula I can be obtained by reaction of a compound of formula II (R<4> is protecting group for carboxyl; X is halogen) with a compound of formula III in a solvent like THF in the presence of a base such as triethylamine.</p> |