| 摘要 |
(3S)-4-(1-Phenylsulfonyl-3-phenyl-2-oxo-2,3-dihydro-1H-indol-3-yl)-mor pholine-3-carboxamide or -3-carboxylate ester derivatives (I) are new. Also new are non-sulfonylated intermediates (II). Indolinone derivatives of formula (I) and their solvates and/or hydrates (including the pure (3R) and (3S) optical isomers at the indole group) are new. R1 = H, 1-4C alkyl, CF3 or OCF3; R2 = H, halo, 1-4C alkyl, 1-4C alkoxy or CF3; or R1+R2 = 5,6-trimethylene; R3 = halo, OH, OMe or OEt; R4 = H, halo, Me, Et, OMe or OEt; or R3+R4 = 2,3-methylenedioxy; R5 = NHEt, NMe2, azetidino, OMe or OEt; R6, R7 = 1-4C alkoxy. Independent claims are also included for: (1) preparation of (I); and (2) new intermediates of formula (II), including their salts with mineral or organic acids, in pure optical isomer or diastereomer mixture form.
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