1,1'-Carbonyldiimidazole → HCID 68843504、化合物

HRID 1725348ノート

反応式

HRID 1725348 の反応式
[F:1][C:2]1[CH:3]=[C:4]([CH:29]=[C:30]([F:32])[CH:31]=1)[O:5][CH2:6][CH2:7][N:8]([CH3:28])[CH2:9][CH2:10][CH2:11][NH:12][CH2:13][C@@H:14]([C:16]1[C:25]2[C:20](=[CH:21][CH:22]=[C:23]([O:26][CH3:27])[CH:24]=2)[N:19]=[CH:18][CH:17]=1)[OH:15].[C:33](N1C=CN=C1)(N1C=CN=C1)=[O:34]>C(Cl)Cl>[F:32][C:30]1[CH:29]=[C:4]([CH:3]=[C:2]([F:1])[CH:31]=1)[O:5][CH2:6][CH2:7][N:8]([CH3:28])[CH2:9][CH2:10][CH2:11][N:12]1[CH2:13][C@@H:14]([C:16]2[C:25]3[C:20](=[CH:21][CH:22]=[C:23]([O:26][CH3:27])[CH:24]=3)[N:19]=[CH:18][CH:17]=2)[O:15][C:33]1=[O:34]

参加物

4

反応物 2

HCID 682631,1'-CarbonyldiimidazoleHCID 44535577(I+/-R)-I+/--[[[3-[[2-(3,5-Difluorophenoxy)ethyl]methylamino]propyl]amino]methyl]-6-methoxy-4-quinolinemethanol

生成物 1

HCID 68843504HCID 68843504、化合物収率 62%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

A mixture of (R)-2-(3-{[2-(3,5-difluoro-phenoxy)-ethyl]-methyl-amino}-propylamino}-1-(6-methoxy-quinolin-4-yl)-ethanol (105 mg, 0.24 mmol), DMAP-(38 mg, 0.31 mmol), 1,1′-carbonyldiimidazole (51 mg, 0.31 mmol) and methylene chloride stabilised on amylene (4 ml) was stirred at room temperature for 16 hours. The solvent was concentrated and the residue was chromatographed on silicagel eluting with methylene chloride-methanol (94-6) to give (R)-3-(3-{[2-(3,5-difluoro-phenoxy)-ethyl]-methyl-amino)-propyl)-5-(6-methoxy-quinolin-4-yl)-oxazolidin-2-one (70 mg, 62%).

後処理

  1. concentrationThe solvent was concentrated
  2. customthe residue was chromatographed on silicagel
  3. washeluting with methylene chloride-methanol (94-6)

出典と根拠

ORDレコード
ord-886f468c26714823bf32312429299622
出典データセット
uspto-grants-2009_02
特許番号
US07491714B2

反応ノート

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