CYCLOALKYLLACTAMIMIDES SUBSTITUES ET PROCEDES DE LEUR PREPARATION

摘要

1328935 Iminoheterocyclic compounds RICHARDSON-MERRELL Inc 12 April 1972 [13 May 1971] 16918/72 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts (which may exist in the form of the tautomeric 2-amino-#1-heterocyclic compounds) wherein Y is thienyl, C 5-7 cycloalkyl or Ph (possibly substituted by halogen or C 1-4 alkyl or alkoxy); Z is H or OH; R and R1 are each H or C 1-4 alkyl, or R1 is halogen; m is 3-6 and n is 3-11. These compounds are prepared by reacting the corresponding substituted cycloalkylamines with (e.g.) an O-methyl-lactim, or with a complex of an appropriate lactam with POCl 3 , COCl 2 , BF 3 -Et 2 O, Me 2 SO 4 and/or hydrogen halide. Starting materials otherwise prepared are 2-pchlorocyclopentanone and 2-hydroxy-2-phenylcyclopentanone and their oximes; and 1-pchlorophenylcyclopentene. Therapeutic compositions having hypoglycemic, hypotensive, anticoagulant and diuretic activity comprise compounds of the above formula, and may be administered orally or parenterally.