4-Methylmorpholine → 2'-Chloro-5'-(2-fluoro-4-morpholin-4-yl-phenylcarbamoyl)-biphenyl-4-carboxylic acid ethyl ester

HRID 1678534ノート

反応式

HRID 1678534 の反応式
[CH2:1]([O:3][C:4]([C:6]1[CH:11]=[CH:10][C:9]([C:12]2[C:17]([Cl:18])=[CH:16][CH:15]=[C:14]([C:19]([OH:21])=O)[CH:13]=2)=[CH:8][CH:7]=1)=[O:5])[CH3:2].[F:22][C:23]1[CH:24]=C(N)[CH:26]=[CH:27][C:28]=1[N:29]1CCOCC1.CCN=C=NCCCN(C)C.C1C=CC2N(O)N=NC=2C=1.[CH3:57][N:58]1[CH2:63][CH2:62][O:61][CH2:60][CH2:59]1>CN(C=O)C.O>[CH2:1]([O:3][C:4]([C:6]1[CH:7]=[CH:8][C:9]([C:12]2[CH:13]=[C:14]([C:19](=[O:21])[NH:29][C:28]3[CH:27]=[CH:26][C:57]([N:58]4[CH2:63][CH2:62][O:61][CH2:60][CH2:59]4)=[CH:24][C:23]=3[F:22])[CH:15]=[CH:16][C:17]=2[Cl:18])=[CH:10][CH:11]=1)=[O:5])[CH3:2]

参加物

8

反応物 5

HCID 79724-MethylmorpholineHCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 757711-HydroxybenzotriazoleHCID 14853303-Fluoro-4-morpholinoanilineHCID 532278844-Chloro-3-(4-ethoxycarbonylphenyl)benzoic acid

生成物 1

HCID 673712232'-Chloro-5'-(2-fluoro-4-morpholin-4-yl-phenylcarbamoyl)-biphenyl-4-carboxylic acid ethyl ester

試薬・触媒・溶媒 2

HCID 962Water溶媒HCID 6228Dimethylformamide溶媒

実験手順

A mixture of 6-chloro-biphenyl-3,4′-dicarboxylic acid 4′-ethyl ester (213 mg), 3-fluoro-4-morpholin-4-yl-phenylamine (179 mg), EDAC (174 mg), HOBT (123 mg) and N-methylmorpholine (200 μl) in DMF (3 ml) was stirred at room temperature. After 11 h, water (30 ml) was added and the resulting suspension filtered. The residue was then purified by chromatography. Elution with 1:1 ethyl acetate:petrol gave a brown oil (235 mg).

後処理

  1. filtrationthe resulting suspension filtered
  2. customThe residue was then purified by chromatography
  3. washElution with 1:1 ethyl acetate

出典と根拠

ORDレコード
ord-2a74595c25314e6dad8db0b72a887e34
出典データセット
uspto-grants-2011_08
特許番号
US08008303B2

反応ノート

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