| 摘要 |
Serine derivatives (I) are new. Serine derivatives of formula (I) are new. R5 = H, 1-4C alkyl, F or Cl; R6 = H, halo or alkyl; R7 = alkyl or cycloalkylalkyl; R8 = OR15 or NR16R17; R9a = H, alkyl, hydroxyalkyl, carboxylalkyl or aminoalkyl; R9b = H or alkyl; R10a = H, F or 1-4C alkyl; R10b = H or F; R11 = H or alkyl; R12 = alkyl, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, cycloalkylalkenyl or cycloalkenylalkenyl (all optionally substituted by 1-3 T); or CR6R12 = cycloalkyl (optionally substituted by 1-3 halo, OH or alkoxy); T = halo, OH, alkoxy, fluoroalkoxy, aryloxy, alkanoyloxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, arylaminosulfonyl, heteroarylaminosulfonyl, heterocyclylaminosulfonyl, aminocarbonylamino, or alkoxycarbonylamino; R15 = H or COR18; R16 = H or alkyl; R17 = H, alkyl, aryl, heteroaryl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, or arylaminosulfonyl; R18 = alkyl (optionally substituted by 1-2 halo, OH, alkoxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, dialkylaminocarbonyl, amino, alkylamino, dialkylamino, alkoxycarbonylamino, alkoxycarbonylalkylamino, aryl or heteroaryl); Ring A = heterocyclic ring (optionally substituted by 1-3 halo, alkyl, CF3, OCF3, NO2, amino, alkylamino, dialkylamino, OH, alkoxy, alkanoyloxy, carboxy, alkoxycarbonyl, azido or alkoxycarbonylamino); E = 1-6C alkylene; and dotted line = optional double bond. An Independent claim is also included for the preparation of (I).
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