| abstract |
Cycloalkano-indole derivs. and aza analogues of formula (I) and isomers and salts are new. R1-C=C-R2 = phenyl, pyridyl or a gp. of formula (a), all opt. substd. by 1-3 gps. R'; R8 = H or 1-4C alkyl; R3-C=C-R4 = phenyl, 4-8C cycloalkene or 4-8 membered oxocycloalkane (all opt. substd. by 1-3 gps. R'); R' = independently halo, CF3, COOH, OH, up to 6C alkoxy carbonyl, 1-6C alkoxy, or 1-6C alkyl (opt. substd. by OH or 1-4C alkoxy); R = H, 4-12C cycloalkyl or 1-12C alkyl; A = CO or CS; X = O, S or NR9; R9 = H or 1-6C alkyl (opt. substd. by OH or phenyl); R5 = phenyl or 5-8 membered, opt. unsatd. heterocyclic with 1-3 heteroatoms (S, N and/or O), (both opt. mono- to tri-substd. by NO2, COOH, halo, CN, 2-6C alkenyl, 1-6C alkoxy or alkyl (opt. substd. by OH, COOH, 1-6C alkoxy or up to 6C alkoxycarbonyl; and/or opt. mono- substd. by OR10 or NR11R12); R10 = H, 1-6C alkyl or 2-6C alkenyl; R11, R12 = H, phenyl, 1-6C alkyl, or up to 8C acyl (opt. subst. by NR13R14); R13, R14 = H or up to 8C acyl; R7 = H; R6 = H, COOH, 1-5 alkoxy, or 1-6C alkyl (opt. substd. by OH or OCOR15); or R6+R7 = O; R<15> = phenyl (opt. mono- to tri-substd., by halo, OH or 1-5C alkyl), or 1-22C alkyl or 2-22C alkenyl (both opt. substd. by OR16); R16 = H, benzyl, triphenylmethyl or up to 6C acyl. Also claimed are intermediates of formula (II). |