To obtain the subject compound useful as an angiotensin II antagonistic agent, etc., in a high yield while forming little by-products by dissolving an imino ether hydrochloride in an organic solvent and adding the solution to ammonia, etc.
The objective compound (e.g. valeroamidine hydrochloride) of formula II is produced by dissolving an imino ether hydrochloride of formula I (R1 is H or a 1-4C alkyl; R2 is methyl or ethyl) in an organic solvent (e.g. methanol) and adding the solution to ammonia or an ammonia solution. Concretely, e.g. 140-160 pts.wt. of an imino ether hydrochloride is dissolved in 15.2-758 pts.wt. of a solvent, separately dissolving 1.0-3.0 times mol (based on the HCl used in the synthesis of the hydrochloride) of ammonia in methanol, adding the hydrochloride solution to the ammonia solution and aging the mixture at a temp. of 5-20°C for 15min to 5.0hr.
YASUI KATSURO
TAKAHARA TETSUYA
Next Patent: PRODUCTION OF ISOCYANATE REACTION PRODUCT