Potassium Carbonate → 4-(7-Azaindol-5-yloxy)-6-benzyloxy-7-methoxyquinazoline

HRID 916386ノート

反応式

HRID 916386 の反応式
[CH2:1]([O:8][C:9]1[CH:10]=[C:11]2[C:16](=[CH:17][C:18]=1[O:19][CH3:20])[N:15]=[CH:14][N:13]=[C:12]2Cl)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[OH:22][C:23]1[CH:24]=[C:25]2[C:29](=[N:30][CH:31]=1)[NH:28][CH:27]=[CH:26]2.C(=O)([O-])[O-].[K+].[K+]>CN(C=O)C>[NH:28]1[C:29]2[C:25](=[CH:24][C:23]([O:22][C:12]3[C:11]4[C:16](=[CH:17][C:18]([O:19][CH3:20])=[C:9]([O:8][CH2:1][C:2]5[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=5)[CH:10]=4)[N:15]=[CH:14][N:13]=3)=[CH:31][N:30]=2)[CH:26]=[CH:27]1

参加物

5

反応物 3

HCID 11430Potassium CarbonateHCID 114265806-(Benzyloxy)-4-chloro-7-methoxyquinazolineHCID 220307221H-Pyrrolo[2,3-b]pyridin-5-ol

生成物 1

HCID 666467954-(7-Azaindol-5-yloxy)-6-benzyloxy-7-methoxyquinazoline収率 60.6%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

A solution of 6-benzyloxy-4-chloro-7-methoxyquinazoline (0.449 g, 1.49 mmol), (EP1153920 production examples 28-30), 5-hydroxy-7-azaindole (0.22 g, 1.64 mmol) and potassium carbonate (0.28 g, 2.02 mmol) in DMF (5 ml) was stirred at 95° C. for 3 hours. The mixture was filtered and the filtrate was evaporated and dried overnight under vacuum. The residue was triturated under methylene chloride and ethyl acetate and the solid was filtered and dried under vacuum to give 4-(7-azaindol-5-yloxy)-6-benzyloxy-7-methoxyquinazoline (0.36 g, 60%).

後処理

  1. filtrationThe mixture was filtered
  2. customthe filtrate was evaporated
  3. customdried overnight under vacuum
  4. customThe residue was triturated under methylene chloride
  5. filtrationethyl acetate and the solid was filtered
  6. customdried under vacuum

出典と根拠

ORDレコード
ord-be113b8b1d4c4147b66c326ff44e1801
出典データセット
uspto-grants-2007_09
特許番号
US07268230B2

反応ノート

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