| 摘要 |
7-Aza-indole-3-carboxamides or glyoxylamides (I) are new. 7-Aza-indoles of formula (I), including their acid or base addition salts, quaternary salts, D-, L- or D,L-isomers and diastereomers, are new: n = 1 or 2; R1 = 1-10C alkyl or 2-10C alkenyl (both optionally substituted (os) by one or more of OH, SH, NH2, NHT, NT2, NHAr, NAr2, NTAr, NO2, CN, halo, OT, OAr, ST, SAr, SO3H, SO2T, SO2Ar, OSO2T, OSO2Ar, COOH, 2-6C alkanoyl, Car or Het); Car = mono-, bi- or tricyclic, 3-14 membered saturated or mono- or polyunsaturated carbocycle (os by one or more R4); Het = mono-, bi- or tricyclic, 5-14 membered saturated or mono- or polyunsaturated heterocycle containing 1-6 heteroatoms (preferably N, O or S) (os by one or more R4); R2, R3 = H (but not both H), 1-5C alkyl (os by one or more of OH, SH, NH2, NHT, NT2, NO2, CN, halo, OT, ST, Ph and pyridyl), phenyl (os by one or more of OH, SH, NH2, NHU, NU2, NO2, CN, COOH, COOU, F, Cl, Br, OU and SU), pyridyl (os by one or more of NO2, CN, COOH, COOU, Cl, Br, OU and SU), halo, OT, ST, Ph and pyridyl), 2,4-dioxo-1,2,6-trimethyl-1,2,3,4-tetrahydropyrimidin-5-yl, 2,4-dioxo-4,6-dimethyl-1,2,3,4-tetrahydropyrimidin-5-yl, 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidin-5-yl or 4H-1,2,4-triazol-3-yl; or NR2R3 = morpholino, thiomorpholino, S,S-dioxo-thiomorpholino or 4-methyl-piperazino; R4 = H, OH, SH, NH2, NHT, NT2, NHAr, NAr2, NTAr, NHCOT, NO2, CN, COOH, COOT, COT, CST, halo, OT, OAr, ST, SAr, SOT or SO2T; T = 1-6C alkyl; Ar = 6-14C aryl; U = 1-3C alkyl. Independent claims are included for the preparation of (I). |
