3-Substd. phenyl-5-hydroxymethyl-furan-2-one derivs. - useful as antidepressants and for treating senility, and their precursors

摘要

Furanone derivs. of formula (I) are new. In (I) R is H and X Y is then CH2CH2, and R1 is 3-methylbutoxy, cyclohexylmethoxy, metanitrobenzyloxy (MNB), MNB-A, MNB-B, metacyanobenzyloxy or 3-cyano-5-nitrobenzyloxy (CNB) or R is acetyl, X Y is CH2CH2 and R1 is MNB-A or MNB-B; or R is CH3 and (a) X Y is CH2CH2 and R1 is 4-chlorobutoxy, 4-chlorobutoxy-B, 4-cyanobutoxy, benzyloxy, benzyloxy-B, MNB, MNB-A, MNB-B, meta-chlorobenzyloxy (MCB), MCB-A, MCB-B, meta-cyano benzyloxy (MCyB), MCyb-A, MCyB-B, 3-methoxypyridine, CNB, CNB-A, CNB-B, 3-chloro-4-fluorobenzyloxy (CFB), CFB-A or CFB-B; (b) X Y is C=CH, R1 is then MNB, MCB, MCyB, benzyloxy or CFB. (I) are reversible inhibitors of monoamine oxidase so are useful as antidepressants and in treating senile cerebral insufficiency. Most cpds. have acute oral LD50 in mice >2g/kg.