2-OXO AND 2-THIO-1,2-DIHYDROQUINOLINYL-OXAZOLIDINONES

摘要

2-(Oxo or thio)-1,2-dihydroquinolinyl-oxazolidinones (I) and their isomers and salts are new: A = O or S; D = H; 3-6C cycloalkyl; alkoxycarbonyl with up to 4C; alkyl or alkenyl with up to 9C optionally substituted by CN, CF3, halo, OH, pyridyl, Ph, COOH, CONH2, alkoxycarbonyl with up to 5C, naphthyl, 3-6C cycloalkyl and/or -(CO)a-NR<2>R<3>, -N(R<4>)-SO2-R<5>, -SO2-N-R<6>R<7> or -S(O)b-R<8>; acyl with up to 5C optionally substituted by CF3, CCl3 or OR<9>; -(CT)d-NR<10>R<11>; -(CO)e-NR<12>-CO-NR<13>R<14>; -NR<15>-SO2R<16>R<17>R<18>-N-SO2-; R<19>-S(O)f; or -CO-R<20>; E, L = H; COOH; halo; CN; CHO; CF3; NO2; or 1-4C alkyl; R<1> = N3; OH; OR<21>; OSO2R<22>; or NR<23>R<24>; a, d, e = 0 or 1; f, b = 0-2; R<2>-R<4>, R<6>, R<7> = H; 1-5C alkyl; or Ph; or NR<2>R<3> = morpholinyl, thiomorpholino, pyrrolidinyl, piperazinyl or piperidyl optionally substituted on a free N atom by alkyl or acyl with up to 4C; R<5>, R<8> = 1-6C alkyl, Ph; benzyl; or tolyl; R<9> = H or 1-5C alkyl optionally substituted by Ph or naphthyl; T = O or S; R<10>-R<15>, R<17>, R<18> = as R<2>-R<4>; R<16>, R<19> = = R<5> and R<8>; R<20> = 6-10C aryl optionally substituted by halo; R<21> = acyl with up to 6C or a OH protecting group; R<22> = 1-5C alkyl; Ph; or toluoyl; R<23>, R<24> = H; 3-6C cycloalkyl; Ph; 1-6C alkoxy; t-Boc; Fmoc; benzyloxycarbonyl; 1-6C alkyl optionally substituted by CN or alkoxycarbonyl with up to 4C; -CT-R<25>; P(O)(OR<26>)(OR<27>) or -SO2-R<28>; R<25> = H; 3-6C cycloalkyl; CF3; 1-6C alkoxy; Ph; Ph-CH2O; 1-6C alkyl optionally substituted by alkoxycarbonyl with up to 5C, CN, F, Cl, Br or CF3; thioalkyl or acyl with up to 5C; or -NR<29>R<30>; R<26>, R<27> = H or 1-4C alkyl; R<28> = 1-4C alkyl or Ph; and R<29>, R<30> = H; Ph; or 1-4C alkyl.