| 摘要 |
4-Amino-chroman (or thiochroman) 8-carboxamide derivatives (I) are new. Novel intermediates are also claimed. (Thio)chromans of formula (I), in racemic or stereoisomeric form, and their salts are new. R1 = (i) -COCH(NH2)CH2SH, (ii) -CH2CH(NH2)CH2SH or (iii) -CH(R11)(R12); R2 = H, alkyl, aralkyl, aryl, alkylcarbonyl, aralkylcarbonyl, arylcarbonyl or heteroarylalkyl; R3 = H, halo, alkyl, aryl or aralkyl; R4 = -CH(R13)(R14); R5 = H or -C(O)-R15; R6-R8, R12 = H, alkyl, aryl or aralkyl; X = O, S, SO or SO2; R11 = heterocyclyl (optionally substituted by one or more of halo, alkyl (optionally mono- or disubstituted by phenyl), alkoxy, alkylthio, cycloalkylalkyl, or aralkyl or heteroarylalkyl (both optionally ring substituted by one or more of halo, alkyl, alkoxy, CN, NO2, amino (optionally substituted by alkylcarbonyl), alkylsulfonyl, polyfluoroalkyl, polyfluoroalkoxy, polyfluoroalkylthio, aryl or heteroaryl (optionally substituted by one or more of halo, alkyl or alkoxy), aralkyl or aryloxy)); R13, R14 = H; or aryl or heteroaryl (both optionally substituted by one or more of halo, alkyl, alkoxy, OH, NO2, NH2, polyfluoroalkoxy or aralkoxy); provided that R13 and R14 are not both H; R15 = OH, alkoxy, amino, aralkylamino, alkylamino or -NHCH(COOR16)(CH2)2SCH3; R16 = H or alkyl. Independent claims are included for the novel intermediates of formula (II) and (XIV); and for the preparation of (I), (II) (or their protected derivatives) and esters of (XIV).
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