| abstract |
Cyclopentane- or cyclopentene-beta-aminoacid derivs. of formula (I) and their isomers, acid addn. salts and metal salt complexes are new: A, B, D, E, G, L, M, T = H (but not all H), halogen, benzyl, OH or 1-8C alkyl (opt. substd. by 1 or 2 of halogen, OH, K, benzyloxy, COOH, 1-6C alkoxy, up to 6C acyl, 2-6C alkoxycarbonyl or -NR4R5); or (i) B+D, E+G or L+M = =CR6R7 or =N-OH; (ii) E+G and/or B+D = O or S; or (iii) B+E or E+M = additional bond, provided that if B+E = bond then D and G are not both H; R4,R5 = H, phenyl or 1-6C alkyl; R6,R7 = H, halogen, 1-8C alkyl, 1-8C alkoxy, up to 8C oxyacyl, benzyl or phenyl; R2 = H; amino-protecting gp.; 1-8C alkyl (opt. substd. by 1 or 2 of OH, CHD, up to 6C acyl, phenyl and benzoyl, the last two themselves opt. substd. by 1 or 2 of halogen, NO2, CN and 1-6C alkyl); up to 8C acyl; benzoyl (opt. substd. as above); -SO2R8; phenyl (opt. susbtd. by 1-3 of halogen, OH, NO2, CF3, OCF3, 1-6C alkyl, up to 6C acyl, 1-6C alkoxy, up to 6C alkoxycarbonyl, NR4R5 or SO2R8); or -COCHR9NHR10; R8 = 1-8C alkyl, or benzyl or phenyl (both opt. substd. by 1-3 of halogen, OH, NO2, CN, CF3, OCF3, 1-6C alkyl, 1-6C alkoxy, up to 6C alkoxycarbonyl, COOH or -NR4R5); R9 = 3-8C cycloalkyl, 6-10C aryl, H or 1-8C alkyl (opt. substd. by CN, MeS, OH, SH, guanidyl, NR11R12, -COR13, 3-8C cycloalkyl or 6-10C aryl (itself opt. substd. by OH, NO2, 1-8C alkoxy, halogen or NR11R12)); R11,R12 = H, 1-8C alkyl or Rh; R13 = OH, benzyloxy, 1-6C alkoxy or -NR10R11 (sic); R10 = H or amino-protecting gp.; R3 = H or 1-8C alkyl (opt. substd. by phenyl); or R2+R3 = =CHR14; R14 = H or 1-8C alkyl (opt. substd. by halogen, OH, Rh, COOH, 1-6C alkoxy or up to 6C alkoxycarbonyl); V = O, S or NH; R1 = H or 1-8C or phenyl (both opt. substd. by 1-3 of OH, halogen, NO2, CN, COOH, CF3, OCF3, 1-6C alkoxy, NR4R5, SO2R8 or (for phenyl only) 1-6C alkyl, up to 6C acyl or up to 6C alkoxycarbonyl); if V = NH, then R1 can also be SO2R8. |