| 摘要 |
2-(Indolecarboxamido)-4-phenyl-thiazole derivatives (I) are new. Thiazole derivatives of formula (I) and their salts and solvates are new: R1 = 2-(R4)-3-(R5)-4-R6-6-methoxyphenyl; R2 = -CH2R7, -(CH2)2R7, -SCH2R7, -CH2-S-R7 or 5-8C alkyl; R3 = indol-2-yl or pyrrolo-pyridyl group of formula (i) or (ii); one of X1-X4 = N and the others = R14; R4 = H or OMe; R5 = H, Me, Et, OMe, OEt or halo; R6 = H, Me, Et, OMe or halo; or R5+R6 = OCH2O; provided that R4-R6 do not all = H; R7 = 5-7C cycloalkyl (optionally substituted by 1 or 2 Me); R8 = -(CH2)n-R15 or -(CH2)m-C6H4-R15; R9 = H or Me; R10-R13 = H, Me, Et, OMe, OEt, SMe, SEt, CF3, NH2 or halo; R14 = H or OMe; R15 = COOH or COOR16; R16 = 1-4C alkyl; n = 1-5; m = 0 or 1. Independent claims are included for the preparation of (I); and for the preparation of carboxylic acid intermediates of formula (XIII), by protecting the amino function of an amine of formula (XI) by treatment with tert. butyl dicarbonate, treating the N-tert. butoxycarbonyl amine product with an alkyl lithium (e.g. n-BuLi or sec. BuLi), condensing the lithiated derivative with an oxalate ester (e.g. ethyl or benzyl oxalate), cyclizing in an acidic medium and saponifying an obtained ester of (XIII) or hydrogenolyzing an obtained benzyl ester of (XIII). X'1-X'4 = CH or CMe; or one = N and the other three = CR14.
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