1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → N-(3,4,5-Trimethoxyphenyl) 3-(5-Methyl-3-(2-fluoro-phenyl)isoxazol-4-oyl)aminophenyl Acetamide

HRID 434030

反応式

HRID 434030 の反応式
CO[C:3]([C:5]1[C:6]([C:11]2[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=2[F:17])=[N:7][O:8][C:9]=1[CH3:10])=[O:4].CCN=C=NCCCN(C)C.[NH2:29][C:30]1[CH:31]=[C:32]([CH2:36][C:37]([NH:39][C:40]2[CH:45]=[C:44]([O:46][CH3:47])[C:43]([O:48][CH3:49])=[C:42]([O:50][CH3:51])[CH:41]=2)=[O:38])[CH:33]=[CH:34][CH:35]=1>C(Cl)Cl.CN(C1C=CN=CC=1)C>[CH3:47][O:46][C:44]1[CH:45]=[C:40]([NH:39][C:37](=[O:38])[CH2:36][C:32]2[CH:33]=[CH:34][CH:35]=[C:30]([NH:29][C:3]([C:5]3[C:6]([C:11]4[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=4[F:17])=[N:7][O:8][C:9]=3[CH3:10])=[O:4])[CH:31]=2)[CH:41]=[C:42]([O:50][CH3:51])[C:43]=1[O:48][CH3:49]

参加物

6

反応物 3

HCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 18756260HCID 18756260、化合物HCID 18756272Methyl 3-(2-fluorophenyl)-5-methylisoxazole-4-carboxylate

生成物 1

HCID 59119375N-(3,4,5-Trimethoxyphenyl) 3-(5-Methyl-3-(2-fluoro-phenyl)isoxazol-4-oyl)aminophenyl Acetamide収率 62%

試薬・触媒・溶媒 2

HCID 142844-(Dimethylamino)pyridine触媒HCID 6344Dichloromethane溶媒

実験手順

To a solution of 4-methoxycarbonyl-5-methyl-3-(2-fluorophenyl)isoxazole (1.00 g, 4.52 mmol) in CH2Cl2 (30 ml) was added EDCI (1.51 g, 9.04 mmol), DMAP (0.11 g, 0.90 mmol), and 2-(3-aminophenyl)-N-(3,4,5-trimethoxyphenyl)acetamide (1.70 g, 5.42 mmol). The reaction was allowed to stir for 6 h then applied to a silica gal column eluting first CH2Cl2 with followed by 10% acetone in CH2Cl2 to give the title compound (1.44 g, 62%).

後処理

  1. washeluting first CH2Cl2

出典と根拠

ORDレコード
ord-64a2ecb7eb564e76a9891605b47c3b09
出典データセット
uspto-grants-2003_12
特許番号
US06670373B1

関連ノート

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