OPTICALLY ACTIVE AMINOPYRIDINE DERIVATIVE AND ITS USE

摘要

PURPOSE:To obtain the subject new derivative useful for preventing and treating hypertension, having strong and durable vasodepressor activity, having extremely low toxicity, comprising an N-(6-amino-3-pyridyl)-N'-(2-norbornyl)guanidine. CONSTITUTION:A 2,5--diaminopyridine of formula I (R1 and R2 are H, 1-6C alkyl or amino-protecting group) is reacted with an optically active-(1S,2R,4R)-2- norbornyl isothiocyanate of the formula R-NCS [R is group of formula II (R3 is H or 1-6C alkyl; (m is 1 or 2) to give an optically active N-(6-amino-3-pyridyl)- N'-[(1S,2R,4R)-2-norbornyl]thiourea of formula III, which is treated with mercury oxide and sulfur powder under reflux to give a carbodiimide derivative of formula IV. This derivative is reacted with NH2CN and optionally oxidized to give an (+)-antipode (salt) of an aminopyridine derivative of formula V (Z is S or NCN; n is 0 or 1).