Morpholine → 4-(4-(2-Carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-morpholinopyrimidine-5-carboxamide

HRID 1986110ノート

反応式

HRID 1986110 の反応式
[C:1]([C:4]1[CH:9]=[C:8]([O:10][C:11]2[CH:16]=[CH:15][C:14]([NH:17][C:18]3[C:23]([C:24]([NH:26][C:27]4[CH:32]=[CH:31][C:30]([F:33])=[CH:29][C:28]=4[F:34])=[O:25])=[CH:22][N:21]=[C:20](S(C)(=O)=O)[N:19]=3)=[CH:13][C:12]=2[F:39])[CH:7]=[CH:6][N:5]=1)(=[O:3])[NH2:2].[NH:40]1[CH2:45][CH2:44][O:43][CH2:42][CH2:41]1>C1COCC1>[C:1]([C:4]1[CH:9]=[C:8]([O:10][C:11]2[CH:16]=[CH:15][C:14]([NH:17][C:18]3[C:23]([C:24]([NH:26][C:27]4[CH:32]=[CH:31][C:30]([F:33])=[CH:29][C:28]=4[F:34])=[O:25])=[CH:22][N:21]=[C:20]([N:40]4[CH2:45][CH2:44][O:43][CH2:42][CH2:41]4)[N:19]=3)=[CH:13][C:12]=2[F:39])[CH:7]=[CH:6][N:5]=1)(=[O:3])[NH2:2]

参加物

4

反応物 2

HCID 8083MorpholineHCID 577213594-(4-(2-carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-(methylsulfonyl)pyrimidine-5-carboxamide

生成物 1

HCID 577213694-(4-(2-Carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-morpholinopyrimidine-5-carboxamide収率 75%

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

To a suspension of 4-(4-(2-carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-(methylsulfonyl)pyrimidine-5-carboxamide (75 mg, 0.13 mmol) in THF (4 mL) was added morpholine (100 mg, 1.1 mmol) and the reaction mixture was stirred 15 min. The solvent was removed in vacuo and the resulting solid was triturated in methanol/ether to give the desired product (55 mg, 75%) as a white solid. MS(ESI+) m/z 566 (M+H)+.

後処理

  1. customThe solvent was removed in vacuo
  2. customthe resulting solid was triturated in methanol/ether

出典と根拠

ORDレコード
ord-a5424d99b370422fbed424b930b68084
出典データセット
uspto-grants-2009_06
特許番号
US07547782B2

反応ノート

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