| 摘要 |
Carboxamidothiazole derivatives (I), their salts and solvates, are new. Carboxamidothiazole derivatives of formula (I), their salts and solvates, are new. R1 = 2-(R4)-3-(R5)-4-(R6)-6-methoxy-phenyl; R2 = CH2-R7, (CH2)2-R7, S-CH2-R7, CH2-S-R7, or 5-8C alkyl; R3 = indol-2-yl of formula (i) or pyrrolo-pyridyl of formula (ii); one of X1, X2, X3, X4 is N and the others = CR14; R4 = H or MeO; R5 = H, Me, Et, i-Pr, MeO, EtO or halo; R6 = H, Me, Et, MeO or halo; or R5+R6 = methylenedioxy; provided that R4, R5, R6 do not all = H; R7 = 5-7C cycloalkyl (optionally substituted by one or two Me); R8 = (CH2)nR15 or -(CH2)m-Ph (ring substituted by R15) R9 = H or Me; R10-R13 = H, Me, Et, OH, acetyloxy, MeO, EtO, methylthio, CF3, amino or halo; R14 = H or MeO; R15 = COOH or COOR16; R16 = 1-4C alkyl; n = 1-5; m = 0 or 1. An Independent claim is included for the preparation of intermediates of formula (XVIII) comprising protecting the amine function of a compound of formula (XIX) with di-tert.-butyldicarbonate, followed by treatment of the resulting compound of formula (XX) with n-BuLi or sec-BuLi, condensing the lithiated derivative with an oxalic ester such as ethyl or benzyl oxalate, followed by saponification of the resulting ester of formula (XXI) in which A is an ethyl or hydrogenating the ester when A is benzyl. X1'- X4' = CH (optionally substituted by methyl); or one of X1'- X4' = N and the others are CR14; R14 = H or MeO.
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