| 摘要 |
5-beta-Acylamido methyl-3-(benzo -diazolyl or -triazolyl) oxazolidin-2-one derivs. of formula (I) and their salts are new. R1 = H, 1-12C alkyl (opt. substd.), 3-12C cycloalkyl, 5-12C alkenyl, phenyl (opt. substd. by 1-3 substits. from OH, OMe, OEt, nitro, F, Cl, Br, COOH, or SO3H), NR11R12, furanyl tetrahydrofuranyl, 2-thiophenyl, pyrrolidinyl, pyridinyl, OR13, amino, NHR13, NR13R14, CH2OH CH2OR15, or COR16; R11, R12 = H or 1-2C alkyl; R13 = 1-4C alkyl; R14 = 1-3C alkyl; or NR13R14 = a 5-7 membered satd. ring opt. including O (morpholine); R15 = 1-4C alkyl; R16 = 1-4C alkyl or phenyl; two of R2-R4 = H; the other = H, halo, 1-6C alkyl, OH, COOR21, OR21, COOH or its anion, CHO, CONHR22R23, CN, C=CH, NC, CHOHMe, Ac, SH, SOMe, SOPh, SMe, SPh, SO2Me, SO2Ph, SO3H, SO2NH2, N3, NO2, NR24R25, NHCOR26, NHCONH2, vinyl, allyl, CH=NOH, CH=NOMe, CMe=NOH, CMe=NOMe or oxiranyl; R21, R26 = 1-4C alkyl or phenyl; R22-R25 = H or 1-3C alkyl; or NR22R23 = a 2-6C satd. ring opt. contg. O; W1.W2 = NR5N=CR6, NR5CR66=N or NR5N=N; R5 = H, 1-12C alky, benzyl, phenethyl, 3-7C cycloalkyl, 2-12C alkenyl contg. 1-3 double bonds, 2-12C alkynyl, CHO, COOR51, COCH2CN, COCH2OH, COCH2OPh (opt. ring substd. by 1-3 OMe), 1 NO2 or 1 NH2), COCH2OR510, phenyl (opt. substd. by 1-2 OMe, 1 NO2 or 1 NH2), COR511, COCH(NHCOR512)R513, or COCH(NH2)NR514, SO2Me, SO2PH or SO3H. R6 = H or 1-3C alkyl; R66 = H, 1-6C alkyl, SH, SM, SEt, SPh, SOMe, SOPh, SO2Me, or SO2Ph; R51 = 1-6C alkyl (opt. substd.by 1 of OMe, COOH, NH2, SO3H, or 1-3 of Cl), 3-7C cycloalkyl, 2-pyridinyl, 2-thienyl, 2-thienylmethyl, 2-pyrrolyl, or phenyl (opt. substd. by 1-3 of Z or COOR58); Z = halo, 1-6C alkyl, OH, COOR52, OR52, COOH, CONR53R54, CN, CHOHMe, Ac, SH, SOMe, SOPh, SMe, SPh, SO2Me, SO2Ph, SO3H, SO2NH2, N3, NO2, NR55R56, or NHCOR57; R52 = 1-4C alkyl or phenyl; R53-R56 = H or 1-3C alkyl; or NR53R54 = a 3-6C satd. ring, opt. contg. O; R57 - 1-4C alkyl or phenyl; R58 - 1-4C alkyl or phenyl (both opt. substd. by Z or CON(R59)2); R59 = H or R58; or N(R59)2 = a 3-6C satd. ring opt. contg. O; R510 = 1-6C alkyl; R511 = 1-6C alkyl, Ph obtd. substd. etc.; R512 = 1-6C alkyl, Ph opt. substd. etc.; R513 = H or CH3; R514 = CH(CH3)2, CH2OH, CH2Ph, CH2COOH, etc.
|
