PURPOSE: To provide a method for producing the subject compound having an excellent vasopressin-antagonizing action, useful as a vasopressin-antagonizing agent, low in side effects, and long in the persistent time of the medicinal effect.
CONSTITUTION: A 2,3-dihydro-1H-benzoazepine derivative of formula I (R1 is H, a halogen; R2 is H, a lower alkyl; R3 is a lower alkyl) is oxidized in the presence of an oxidizing agent and a cooxidizing agent in a proper solvent at 0-70°C, preferably 0-50°C, to obtain the 2,3,4,5-tetrahydro-1H-benzoazepine derivative of formula II. Or, the epoxide of a 2,3,4,5-tetrahydro-1H-benzoazepine derivative of formula III is cleaved to obtain a 2,3,4,5-tetrahydro-1H-benzoazepine derivative of formula IV. The compounds of formulas I and III as starting materials also have the same excellent vasopressin-antagonizing action as those of the objective components of formula II and IV, and useful as a vasodilator, an antihypertensive, a water diuretic agent, a platelet aggregation-inhibiting agent, etc.
OTANI NAOAKI
MORITA SEIJI
MATSUBARA ATSUSHI
UCHIDA MINORU
YAMASHITA SHUJI
