PURPOSE: To easily produce the subject compound exhibiting K+ channel opening effect and having hypotensive action and coronary vasodilating action in a short time by treating an amide compound with a dehydrative condensation agent and reacting with cyanamide.
CONSTITUTION: An N-cyano-N'-substituted-arylcarboxyimidamide compound of formula II can be produced by treating an amide compound of formula I (Ar is phenyl, pyridyl, thienyl, quinolyl or isoquinolyl; R1 is alkyl, OH, phenyl or pyridyl; (n) is 0-4) with a dehydrative condensation agent such as acetic anhydride and reacting the product with cyanamide. Especially, an N-cyano-N'- substituted-arylcarboxyimidamide compound of formula IV can be produced from an amide compound of formula III [Ar' is (2-, 3- or 4-)pyridyl which may have amino substituent; R1 is phenylene which may have halogen substituent; (n') is 2] by this process. The starting compound of the formula I is obtained by reacting a carboxylic acid compound of formula V with an amine compound of formula VI.
WO/2002/030881 | SULFONYLGUANIDINE |
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NAKAJIMA YOSHIYA
MUNEZUKA YUUJI