PURPOSE: To obtain the subject new acetonitrile derivative, having a specific aryl group substituted at the α-position of acetonitrile and excellent hypotensive and vasodilator actions and useful as an oral or a parenteral antihypertensive agent for treating hypertension, etc.
CONSTITUTION: A compound expressed by formula I [R1 is H, 1-6C alkyl, etc.; Ar is (substituted)benzene ring; X is the formula (CH2)m ((m)is 0 or 1-3) or CO; Y is 5- or 6-membered ring (substituted) heterocyclic ring, condensed heterocyclic ring, etc.]{e.g. 2-[4-(1,2,4-triazol-5-yl)-phenyl]-propionitrile} is dissolved in tetrahydrofuran. Methyl isothiocyanate is then added to the solution and the above-mentioned compound is reacted with the methyl isocyanate in the presence of potassium tert. butoxide for 2 hr while being cooled with ice. Aqueous hydrochloric acid is subsequently added to neutralize the reaction mixture, which is then extracted with ethyl acetate. The extracted compound is purified by silica gel column chromatography to afford the objective thiocarbamoylacetonitrile derivative expressed by 2 formula II (R2 is 1-10C alkyl).
BESSHO HIDEKI
KIYONO ASAMI
HAYASHI JUNKO
