N-ALKANOYLPHENYLALANINE DERIVATIVES

摘要

N-Alkanoyl-phenylalanine derivatives (I) are new. - Phenylalanine derivatives of formula (I) and their salts and esters are new. One of X, X' = H, halo or alkyl, and the other = amide group of formula (i); or one of X and X' = amide or imidazolidinone group of formula (ii) or (iii); R1 = H or alkyl; R15 = halo, NO2, alkylsulfonyl, CN, OH, alkoxy, alkoxycarbonyl, COOH, alkylaminosulfonyl, perfluoroalkyl, alkyl (optionally substituted with thio, OH, alkoxy, halo, alkylthio, alkylsulfinyl or alkylsulfonyl), alkylsulfinyl, alkanoyl, aroyl, aryloxy or R17-Ctriple boundC-; R16 = H, halo, NO2, CN, alkyl, OH, perfluoroalkyl or alkylthio; R17 = H, aryl, heteroaryl or alkyl (optionally substituted by OH, aryl or heteroaryl); a = 0 or 1; Het = heteroaromatic ring, either 5- or 6-membered and containing 1-3 N, O or S heteroatoms or 9- or 10-membered, bicyclic and containing 1-4 N, O or S; R30 = H or alkyl or is absent; R18 = alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl; R19 = alkyl (optionally substituted by one or more halo, OH, alkoxy, aryl, heteroaryl or alkylthio), aryl or heteroaryl; R20 = alkyl or alkanoyl; or R19 + R20 = (CH2)4; Y = (i) 2-(R22)-6-(R23)-phenyl additionally substituted by R24; or (ii) C-bonded heteroaromatic ring as defined for Het, which is C-substituted by 1 or 2 of alkyl, halo, CN, perfluoroalkyl, at least one substituent being on a C adjacent to the bonding C; R22, R23 = H, alkyl, alkoxy, alkoxyalkyl, alkylamino, aryl, arylalkyl, NO2, CN, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, halo or perfluoroalkyl; at least one of R22, R23 is other than H; R24 = H, OH, alkyl, alkoxy, NH2, aryl, NO2, CN, alkylsulfonyl, halo, -SO2NR25R26, -C(O)NR25R26 or 5-(NR25R26)-1-tetrazolyl; R25 = H, alkyl, aryl, arylalkyl or alkoxyalkyl; R26 = H or alkyl; or R22 + R24 form a fused benzene ring; Z is not defined in claim 1 (preferably H in a subsequent claim); alkyl moieties have 1-6C.