Ammonium formate → 4-(2,3-Dimethylindol-5-yloxy)-7-hydroxy-6-methoxyquinazoline

HRID 454092

反応式

HRID 454092 の反応式
C([O:8][C:9]1[CH:18]=[C:17]2[C:12]([C:13]([O:19][C:20]3[CH:21]=[C:22]4[C:26](=[CH:27][CH:28]=3)[NH:25][C:24]([CH3:29])=[C:23]4[CH3:30])=[N:14][CH:15]=[N:16]2)=[CH:11][C:10]=1[O:31][CH3:32])C1C=CC=CC=1.C([O-])=O.[NH4+]>CN(C=O)C.[Pd]>[CH3:29][C:24]1[NH:25][C:26]2[C:22]([C:23]=1[CH3:30])=[CH:21][C:20]([O:19][C:13]1[C:12]3[C:17](=[CH:18][C:9]([OH:8])=[C:10]([O:31][CH3:32])[CH:11]=3)[N:16]=[CH:15][N:14]=1)=[CH:28][CH:27]=2

参加物

5

反応物 2

HCID 2723923Ammonium formateHCID 220308297-Benzyloxy-4-(2,3-dimethylindol-5-yloxy)-6-methoxyquinazoline

生成物 1

HCID 1357631184-(2,3-Dimethylindol-5-yloxy)-7-hydroxy-6-methoxyquinazoline収率 69.8%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 6228Dimethylformamide溶媒

実験手順

A solution of 7-benzyloxy-4-(2,3-dimethylindol-5-yloxy)-6-methoxyquinazoline (2 g, 4.7 mmol) in DMF (120 ml) containing ammonium formate (11 gr, 174 mmol) and 10% palladium on charcoal (200 mg) was stirred for 2.5 hours at ambient temperature. The mixture was filtered, and the filtrate was evaporated under vacuum. The residue was triturated with ether and the solid was filtered, washed with water followed by ether and dried under vacuum at 50° C. to give 4-(2,3-dimethylindol-5-yloxy)-7-hydroxy-6-methoxyquinazoline (1.1 g, 69%).

後処理

  1. filtrationThe mixture was filtered
  2. customthe filtrate was evaporated under vacuum
  3. customThe residue was triturated with ether
  4. filtrationthe solid was filtered
  5. washwashed with water
  6. customdried under vacuum at 50° C.

出典と根拠

ORDレコード
ord-7218090d733b4b65ac2cc4aa660ad0b1
出典データセット
uspto-grants-2013_07
特許番号
US08492560B2

関連ノート

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