PROCESS FOR PREPARING TETRACYCLIC SPIROHYDANTION DERIVATIVES

摘要

Title compds. I [X=H,F,Cl,CH3; R=H, C1-9alkyl, C2-9alkenyl, C5- 7cycloalkyl, benzyl, pyridyl, 4-hydroxybenzyl, HSCH2-, CH3SCH2-, FCH2, HOCH2-, etc. , useful as an aldose reductase, are prepd. Thus, a mixt. contg. 100mg 8'-amino derivs. of the compd. II, 60mg butyl glyoxylate, 1ml conc. HCl, and 3ml ethanol is stirred at room temp. for 1hr. The resulting yellow solid material is washed with ethanol and ether and dried at 120≦̸C to give 50.54 mg I [R=H (yield=49%).