NEW MATERIAL:A compound shown by formula I [R1 is COOH, CONH2, CN, tetrazolyl or (substituted) aryl; R2 is (substituted) aryl or heterocyclic group; R3 and R4 are H, lower alkyl or (substituted) aryl; n is 0-2; X is O or S; Y is single bond or NH; Z is C(A)H (A is H, halogen or OH) or CP with the proviso that when A is H, R1 is aryl or tetrazolyl and R2 is aryl].
EXAMPLE: (R)-N,N-Di-(n-amyl)-3-carboxyl-2-(n-tolylcarbamoylamino)-propanoic acid amide.
USE: An antagonist against cholecystokinin and gastrin acceptor.
PREPARATION: An ω-2-aminoalkyldicarboxylic acid is protected with a carboxyl protecting group R5 and an amino protecting group R6 to give a compound shown by formula II, which is condensed with a disubstituted amine compound to give a compound shown by formula III. Then the protecting group R6 is removed and then the resulting substance is reacted with an acid chloride to give a compound shown by formula IV, which is deprotected to give a compound shown by formula V.
ISHIHARA TERUICHI
HAGISHITA YAMAJI
SENO KAORU
IHII NOBUHIRO
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