A PROCESS FOR THE PREPARATION OF A BIOLOGICALLY ACTIVE TETRACYCLIC HYDANTOIN DERIVATIVE

摘要

Novel biologically-active tetracyclic spirohydantoin derivatives of formula …… wherein… X is hydrogen, fluorine, chlorine or methyl; and… R is hydrogen, alkyl, alkenyl, cycloalkyl, benzyl, 4-hydroxybenzyl, pyridyl, HSCH2-, CH3SCH2-, CH3SCH2CH2-, FCH2-, HOCH2-, CH2CH(OH)-, CH3CH(OH)CH2-, HOOCCH2-, HOOCCH2CH2-, H2NCOCH2-, H2NCOCH2CH2-, H2NCH2CH2- CH2CH2-, ……H2@@@H-CH2CH2CH2-, …… COOC2H5, -CONH2, CONH(CH2)2OH, -CONH cyclohexyl, -CONH-nBu, -CONH(CH2)3 N(CH3)2, -CON(C2H5)2, …… phenyl or phenyl substituted by chlorine, fluorine, bromine, hydroxy, methyl, methoxy, trifluoromethyl, -COCH3, -N(CH3)2, -SCH3, -SOCH3, -SO2CH3, -COOH, -CONH2, -COOCH3 or -CON Alk, are disclosed. …These derivatives are potent inhibitors of aldose reductase and useful in treating diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.