Morpholine → HCID 69103534、化合物

HRID 2217260ノート

反応式

HRID 2217260 の反応式
[NH2:1][C:2]1[N:3]=[C:4]([C:19]2[CH:24]=[CH:23][CH:22]=[CH:21][CH:20]=2)[C:5]([C:9]2[CH:10]=[CH:11][C:12](=[O:18])[N:13]([CH:15]([CH3:17])[CH3:16])[CH:14]=2)=[N:6][C:7]=1Br.[NH:25]1[CH2:30][CH2:29][O:28][CH2:27][CH2:26]1.CN1C(=O)CCC1.CCOC(C)=O>O>[NH2:1][C:2]1[N:3]=[C:4]([C:19]2[CH:24]=[CH:23][CH:22]=[CH:21][CH:20]=2)[C:5]([C:9]2[CH:10]=[CH:11][C:12](=[O:18])[N:13]([CH:15]([CH3:17])[CH3:16])[CH:14]=2)=[N:6][C:7]=1[N:25]1[CH2:30][CH2:29][O:28][CH2:27][CH2:26]1

参加物

6

反応物 4

HCID 8083MorpholineHCID 8857Ethyl AcetateHCID 13387N-methyl-2-pyrrolidoneHCID 11429076HCID 11429076、化合物

生成物 1

HCID 69103534HCID 69103534、化合物収率 82.7%

試薬・触媒・溶媒 1

HCID 962Water溶媒

反応条件

温度
150 °C

実験手順

A mixture of 5-(5-amino-6-bromo-3-phenyl-2-pyrazinyl)-1-isopropyl-2(1H)-pyridone (100 mg), morpholine (113 mg), and NMP (1.0 ml) was heated at 150° C. with stirring for 1 day. After cooling, EtOAc and water were poured into the mixture, and the organic layer was separated, washed with water and brine, and dried over MgSO4. The solvent was removed under reduced pressure, and the residue was recrystallized from MeOH-IPE and dried in vacuo to give 5-[5-amino-6-(4-morpholinyl)-3-phenyl-2-pyrazinyl]-1-isopropyl-2(1H)-pyridone (84 mg).

後処理

  1. temperatureAfter cooling
  2. customthe organic layer was separated
  3. washwashed with water and brine
  4. dry with materialdried over MgSO4
  5. customThe solvent was removed under reduced pressure
  6. customthe residue was recrystallized from MeOH-IPE
  7. customdried in vacuo

出典と根拠

ORDレコード
ord-fc646ac706ff4999893553499ce78cdb
出典データセット
uspto-grants-2008_08
特許番号
US07407961B2

反応ノート

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