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

HRID 916386노트

반응식

HRID 916386 반응식
[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

참가 물질

5

반응물 3

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

생성물 1

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

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

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%).

후처리

  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

출처 및 근거

ORD 기록
ord-be113b8b1d4c4147b66c326ff44e1801
출처 데이터셋
uspto-grants-2007_09
특허 번호
US07268230B2

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