Hydrochloric Acid → 7-Benzyloxy-4(indol-5-ylamino)-6-methoxyquinazoline hydrochloride

HRID 454197ノート

反応式

HRID 454197 の反応式
[CH2:1]([O:8][C:9]1[CH:18]=[C:17]2[C:12]([C:13]([Cl:19])=[N:14][CH:15]=[N:16]2)=[CH:11][C:10]=1[O:20][CH3:21])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[NH2:22][C:23]1[CH:24]=[C:25]2[C:29](=[CH:30][CH:31]=1)[NH:28][CH:27]=[CH:26]2.Cl>C(O)(C)C>[ClH:19].[CH2:1]([O:8][C:9]1[CH:18]=[C:17]2[C:12]([C:13]([NH:22][C:23]3[CH:24]=[C:25]4[C:29](=[CH:30][CH:31]=3)[NH:28][CH:27]=[CH:26]4)=[N:14][CH:15]=[N:16]2)=[CH:11][C:10]=1[O:20][CH3:21])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1

参加物

5

反応物 3

HCID 313Hydrochloric AcidHCID 788675-AminoindoleHCID 106619987-(Benzyloxy)-4-chloro-6-methoxyquinazoline

生成物 1

HCID 220305477-Benzyloxy-4(indol-5-ylamino)-6-methoxyquinazoline hydrochloride収率 96%

試薬・触媒・溶媒 1

HCID 3776Isopropanol溶媒2 回

実験手順

A solution of 7-benzyloxy-4-chloro-6-methoxyquinazoline (5 g, 16.6 mmol), (prepared as described for the starting material in Example 1), 5-aminoindole (2.4 g, 18.2 mmol) in isopropanol (60 ml) containing 5N hydrogen chloride in isopropanol (260 μl, 1.6 mmol) was refluxed for 90 minutes. After cooling the volatiles were removed under vacuum. The solid was triturated with isopropanol, filtered, washed with isopropanol followed by ether and dried under vacuum to give 7-benzyloxy-4-(indol-5-ylamino)-6-methoxyquinazoline hydrochloride (6.9 g, 96%).

後処理

  1. temperaturewas refluxed for 90 minutes
  2. temperatureAfter cooling the volatiles
  3. customwere removed under vacuum
  4. customThe solid was triturated with isopropanol
  5. filtrationfiltered
  6. washwashed with isopropanol
  7. customdried under vacuum

出典と根拠

ORDレコード
ord-0dcd299550ad4a7cbfd7e8b2cf6dcec5
出典データセット
uspto-grants-2013_07
特許番号
US08492560B2

反応ノート

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