NEW MATERIAL:The compound of formulaI[R1 is 5W6-membered heterocyclic group containing 1W4 hetero atoms (O, S or N); R2WR4 are H or lower alkyl; R4 may be CN, lower alkyl having substituent group (e.g. CN, OH, etc.), lower alkoxycarbonyl, etc.; A is OH, alkoxy, amino which may have substituent group (e.g. alkyl which may be substituted with halogen, etc., OH, etc.), or hydrazino which may have lower alkyl, etc.], and its salt.
EXAMPLE: 2-(2-Cyanoethyl)-N-nicotinoylalanine methyl ester.
USE: An immunoactivating agent and host-interstitial carcinostatic agent.
PROCESS: The reaction of the compound of formula II (M1 is alkyl) with the compound of formula III (X is halogen) or its hydrohalogenic acid salt in the presence of a base gives the compound of formula IV, which is hydrolyzed to obtain the objective compound of formulaI(A is OH).
KITAMURA KOUICHI
SHINKAI KENKICHI
YASUDA HIROSHI