| abstract |
NEW MATERIAL:A derivative of formula I (X1, X2 are H, halogen, lower alkyl, alkoxy; Y is methylene, O, S; R1-R4 are H, lower alkyl, or incorporate to form, together with adjacent ring carbon atoms, a benzene ring) and its salt. EXAMPLE:5',6'-Dihydrospiro[ pyrrolidine-3,1'-( 4H )pyrrolo( 3,2,1-ij )quinoline ]-2, 2',5(1'H)-trione. USE:An aldose reductase inhibitor which is used as a preventive and remedy for a variety of complications with diabetes. Toxicity is extremely low and scarcely shows central inhibition. PREPARATION:The reaction of a compound of formula II (R9 is lower alkyl) with a cyanide gives a compound of formula III, which is subsequently cyclized to give a compound of formula IV, then the product is decarboxylated. |