PURPOSE: To obtain a new indolin-2-one derivative having selective antagonistic action on gastrin receptor without giving side actions caused by CCK-A receptor antagonistic action and useful e.g. for the treatment and prevention of peptic ulcer, gastritis, etc.
CONSTITUTION: This indolin-2-one derivative expressed by the formula III [R2 is same as R2' ; R4 is H, (substituted) lower alkyl, substituted)aryl, etc.; X and Y are CH2, NH or O] is produced by dissolving an isatin derivative expressed by the formula I (R1 is halogen, lower alkyl, lower alkoxy, OH, etc.; n is integer of 0-4) in an inert solvent, reacting with a compound of the formula R2Br [R2' is H, (substituted) lower alkyl, (substituted) lower alkenyl, (substituted) lower alkoxy, etc.] in the presence of a base to obtain an N-substituted isatin derivative expressed by the formula II and successively reacting the product with an orthoformic acid ester and a urea derivative or reacting with H2NOH, H2. and a compound of the formula R3NCO [R3 is (substituted) lower alkyl, (substituted)aryl, etc.], etc.
EMURA TAKESHI (JP)
HOSHINO HIDEKAZU (JP)
