Antihypertensive thio:formamide sulphoxide derivs. - prepd. by electrochemically oxidising ring sulphur atom of corresp. thio:formamide

摘要

Prepn. of a 2-heterocyclyl-2-thioamido tetrahydrothiophene S-oxide or analogue of formula (I) comprises electrochemical oxidn. of a corresp. tetrohydrothiophene or analogue (II), i.e. (I, n is O). Oxidn. is carried out in aq. electrolyte at pH 7-7.5 and in presence of specific oxidising agent X(+) obtd. in situ from halide X(-) electrochemically at an imposed electrode potential similar to the oxidn. potential of X(-). R is H or 1-4C alkyl; Het is pyridin-3-yl (opt. substd. by a 1-4C alkyl or a halogen), quinolin-3-yl, pyridazin-4-yl, pyridimidin-5-yl, thiazol-5-yl, thieno(2,3-b)pyridin-5-yl or thieno (3,2-b)pyridin-6-yl; and Y is a bond or CH2. S-oxidn. is selective for prodn. of (I), which are antihypertensives having LD50 values orally in mice over 300 mg/kg. Dose is 0.02-50 mg/kg. (Provisional Basic previously advised in week 8418).