首页> 外国专利> 5'-Indolinyl-5β-amidomethyloxazolidin-2-ones, 3- (condensed ring-substituted) phenyl-5β-amidomethyloxazolidine-2-ones and 3- (nitrogen atom-substituted) phenyl-5β-amidomethyloxazolidine -2-ones

5'-Indolinyl-5β-amidomethyloxazolidin-2-ones, 3- (condensed ring-substituted) phenyl-5β-amidomethyloxazolidine-2-ones and 3- (nitrogen atom-substituted) phenyl-5β-amidomethyloxazolidine -2-ones

机译:5'-吲哚基-5β-氨基甲基恶唑烷-2-酮,3-(稠环取代)苯基-5β-氨基甲基恶唑烷-2-酮和3-(氮原子取代)苯基-5β-氨基甲基恶唑烷-2-酮

摘要

of formulae (XI) and (XIII), 3-(fused ring substd.)phenyl-5 beta -(amidomethyl)oxazolidin-2-ones of formula (XXI), and 3-(N-substd.)phenyl-5 beta (aminodimethyl)oxazolidin-2-ones of formula (IV), and their salts are new: where in (XI); R1 = e.g. H, 1-12C alkyl (opt. substd. with 1-3 Cl), 3-12C cycloalkyl, 5-12C monosubstd. alkenyl, phenyl furanyl, tetrahydrofuranyl or 2-thiophene etc. 2 of R2, R3, R4 = H and the other = e.g. H, F, Cl, Br, I or 1-6C alkyl etc. R5 = e.g. H, 1-12C alkyl, benzyl, phenethyl, 3-7C cycloalkyl, 2-12C alkenyl contg. 1-3 double bonds, 2-12C alkynyl contg. 1 triple bond, -CHO etc. in (XIII), X1 = Ac, -COOtBn, -COOCH2Ph or -COO(CH2)2SiMe3; R2, R3, R4 = as above; and R6 = I, N3 or NH2; in (XXI), R1 = as above; R2 or R4 = H and the other together with R3 is -(CH2)n3-(CR10-1R10-2)n7 -CO-(CR10-3R10-4)n8-(CH2)n4-, -(CH2)n5-CH=CH-(CH2)n6- or -(CH2)n3-(CR10-1 R10-2)n7-C(:NOR7)-(CR10-3R10-4)n8-(CH2)n4-; n3, n4 = 0-3; n7, n8 = 0 or 1; R10-1, R10-2 = H or 1-3C alkyl or together complete spirocyclopropyl; R10-3, R10-4 = H or 1-3C alkyl or together complete spirocyclopropyl; with the provisos that (1) n7 + n8 = 1 or (b) n7 = 1 and one of R10-1 or R10-2 is not H; n5, n6 = 0-2; n5 + n6 = 1 or 2; R7 = H, 1-4C alkyl, -CH2COOH or -CH2COOR7-1; R7-1 = 1-4C alkyl; R5 or R6 = H and the other is as for R5 in (XI) above; in (IV), R1, R2, R3, R4 = as in (XI); W1 and W2 together = -NR5-N=CR'6-, -NR5-CR''6=N-or -NR5-N=N-; and R5 = as in (XI); R'6 = H or 1-3C alkyl; and R''6 = H, 1-6C alkyl, SH, SMe, Set, SPh, SOMe, SOPh, SO2Me or SO2Ph.
机译:式(XI)和(XIII),式(XXI)的3-(稠环取代)苯基-5β-(酰胺甲基)恶唑烷-2-酮和3-(N-取代的)苯基-5β式(IV)的(氨基二甲基)恶唑烷丁-2-酮及其盐是新的。 R1 =例如H,1-12C烷基(优选用1-3 Cl取代),3-12C环烷基,5-12C单取代。 R 2,R 3,R 4中的2 = H,另一个=例如1,2,3,3,2,3,4,5,5,5,5,7,7亚烷基。 H,F,Cl,Br,I或1-6C烷基等。R5 =例如H,1-12C烷基,苄基,苯乙基,3-7C环烷基,2-12C烯基(续)。 1-3个双键,2-12C炔基(续)。 (XIII)中的1个三键,-CHO等,X1 = Ac,-COOtBn,-COOCH2Ph或-COO(CH2)2SiMe3; R2,R3,R4 =如上所述;并且R6 = I,N3或NH2;在(XXI)中,R1 =以上; R2或R4 = H,另一个与R3一起是-(CH2)n3-(CR10-1R10-2)n7 -CO-(CR10-3R10-4)n8-(CH2)n4-,-(CH2)n5- CH = CH-(CH2)n6-或-(CH2)n3-(CR10-1 R10-2)n7-C(:NOR7)-(CR10-3R10-4)n8-(CH2)n4-; n3,n4 = 0-3; n7,n8 = 0或1; R10-1,R10-2 = H或1-3C烷基或一起完整的螺环丙基; R10-3,R10-4 = H或1-3C烷基或一起完整的螺环丙基;前提是(1)n7 + n8 = 1或(b)n7 = 1并且R10-1或R10-2中的一个不为H; n5,n6 = 0-2; n5 + n6 = 1或2; R7 = H,1-4C烷基,-CH2COOH或-CH2COOR7-1; R7-1 = 1-4C烷基; R5或R6 = H,另一个与上述(XI)中的R5相同。在(IV)中,R 1,R 2,R 3,R 4 =与(XI)相同。 W1和W2一起= -NR5-N = CR'6-,-NR5-CR''6 = N-或-NR5-N = N-;并且R5 =如(XI)中那样; R'6 = H或1-3C烷基;和R''6 = H,1-6C烷基,SH,SMe,Set,SPh,SOMe,SOPh,SO2Me或SO2Ph。

著录项

  • 公开/公告号JP2865211B2

    专利类型

  • 公开/公告日1999-03-08

    原文格式PDF

  • 申请/专利权人 FUARUMASHIA ANDO ATSUPUJON CO;

    申请/专利号JP19890509255

  • 发明设计人 BURITSUKUNAA SUTEIIBUN JEI;

    申请日1989-08-22

  • 分类号C07D263/20;C07D413/04;

  • 国家 JP

  • 入库时间 2022-08-22 02:29:08

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