Water → 2-(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(2,6-difluorophenyl)acetamide

HRID 640011

反応式

HRID 640011 の反応式
[Cl-].COC1C=C(OC)NN([N+]2(C)CCOCC2)N=1.[Cl:19][CH2:20][CH2:21][CH2:22][O:23][C:24]1[CH:33]=[C:32]2[C:27]([C:28]([NH:34][C:35]3[CH:36]=[N:37][N:38]([CH2:40][C:41](O)=[O:42])[CH:39]=3)=[N:29][CH:30]=[N:31]2)=[CH:26][CH:25]=1.[F:44][C:45]1[CH:51]=[CH:50][CH:49]=[C:48]([F:52])[C:46]=1[NH2:47].O>CN(C)C=O>[Cl:19][CH2:20][CH2:21][CH2:22][O:23][C:24]1[CH:33]=[C:32]2[C:27]([C:28]([NH:34][C:35]3[CH:36]=[N:37][N:38]([CH2:40][C:41]([NH:47][C:46]4[C:45]([F:44])=[CH:51][CH:50]=[CH:49][C:48]=4[F:52])=[O:42])[CH:39]=3)=[N:29][CH:30]=[N:31]2)=[CH:26][CH:25]=1

参加物

6

反応物 4

HCID 962WaterHCID 796472,6-DifluoroanilineHCID 68638745(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetic acidHCID 686392154-(4,6-Dimethoxytriazin-2-yl)-4-methylmorpholinium chloride

生成物 1

HCID 686382872-(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(2,6-difluorophenyl)acetamide収率 77%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

4-(4,6-dimethoxytriazin-2-yl)-4-methylmorpholinium chloride (0.391 g, 1.32 mmol) was added in one go, at room temperature, to a stirred suspension of (4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)acetic acid (0.400 g, 1.11 mmol) and 2,6-difluoroaniline (0.171 g, 1.32 mmol) in dimethylformamide (7 ml). The mixture was stirred for 2 hours and then poured into water (30 ml) the resultant solid was filtered to give 2-(4-{[7-(3-chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-1-yl)-N-(2,6-difluorophenyl)acetamide (0.403 g, 77% yield) as a pale brown solid:

後処理

  1. filtrationwas filtered

出典と根拠

ORDレコード
ord-130b738977134dfcb2d3a650e0f990e8
出典データセット
uspto-grants-2010_04
特許番号
US07691867B2

関連ノート

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