Isopropanol → 7-Benzyloxy-4-(4-chloro-2-fluorophenylamino)-6-methoxyquinazoline hydrochloride

HRID 238106

反応式

HRID 238106 の反応式
Br[C:2]1[CH:35]=[CH:34][C:5]([NH:6][C:7]2[C:16]3[C:11](=[CH:12][C:13]([O:19][CH2:20][CH:21]4CCN(C(OC(C)(C)C)=O)[CH2:23][CH2:22]4)=[C:14]([O:17][CH3:18])[CH:15]=3)[N:10]=[CH:9][N:8]=2)=[C:4]([F:36])[CH:3]=1.[Cl:37]C1C=CC(N)=C(F)C=1.[CH3:46][CH:47](O)[CH3:48]>>[ClH:37].[CH2:20]([O:19][C:13]1[CH:12]=[C:11]2[C:16]([C:7]([NH:6][C:5]3[CH:34]=[CH:35][C:2]([Cl:37])=[CH:3][C:4]=3[F:36])=[N:8][CH:9]=[N:10]2)=[CH:15][C:14]=1[O:17][CH3:18])[C:21]1[CH:48]=[CH:47][CH:46]=[CH:23][CH:22]=1

参加物

4

反応物 3

HCID 3776IsopropanolHCID 938984-Chloro-2-fluoroanilineHCID 11049999tert-Butyl 4-(((4-((4-bromo-2-fluorophenyl)amino)-6-methoxyquinazolin-7-yl)oxy)methyl)piperidine-1-carboxylate

生成物 1

HCID 224782657-Benzyloxy-4-(4-chloro-2-fluorophenylamino)-6-methoxyquinazoline hydrochloride収率 64%

実験手順

A solution of 7-benzyloxy-4-chloro-6-methoxyquinazoline hydrochloride (1.2 g, 4 mmol), (prepared as described in WO 97/22596, Example 1), and 4-chloro-2-fluoroaniline (444 μl, 4 mmol) in 2-propanol (40 ml) was heated at reflux for 1.5 hours. After cooling, the precipitate was collected by filtration, washed with 2-propanol then ether and dried under vacuum to give 7-benzyloxy-4-(4-chloro-2-fluoroanilino)-6-methoxyquinazoline hydrochloride (1.13 g, 64%).

後処理

  1. temperatureat reflux for 1.5 hours
  2. temperatureAfter cooling
  3. filtrationthe precipitate was collected by filtration
  4. washwashed with 2-propanol
  5. dry with materialether and dried under vacuum

出典と根拠

ORDレコード
ord-2afa68698b1747778a266f7892b3ef51
出典データセット
uspto-grants-2014_02
特許番号
US08642608B2

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