Ethyl 2-aminopyridine-3-carboxylate → 2-[2-(2,4,6-Trifluorophenyl)-acetylamino]-nicotinic acid ethyl ester

HRID 550357

反応式

HRID 550357 の反応式
[CH2:1]([O:3][C:4](=[O:12])[C:5]1[CH:10]=[CH:9][CH:8]=[N:7][C:6]=1[NH2:11])[CH3:2].[F:13][C:14]1[CH:19]=[C:18]([F:20])[CH:17]=[C:16]([F:21])[C:15]=1[CH2:22][C:23](Cl)=[O:24]>C1(C)C=CC=CC=1.C(OCC)C>[CH2:1]([O:3][C:4](=[O:12])[C:5]1[CH:10]=[CH:9][CH:8]=[N:7][C:6]=1[NH:11][C:23](=[O:24])[CH2:22][C:15]1[C:16]([F:21])=[CH:17][C:18]([F:20])=[CH:19][C:14]=1[F:13])[CH3:2]

参加物

5

反応物 2

HCID 12433260Ethyl 2-aminopyridine-3-carboxylateHCID 574280152,4,6-Trifluorophenylacetyl chloride

生成物 1

HCID 586172322-[2-(2,4,6-Trifluorophenyl)-acetylamino]-nicotinic acid ethyl ester収率 93%

試薬・触媒・溶媒 2

HCID 1140Toluene溶媒2 回HCID 3283Diethyl Ether溶媒

実験手順

2-Aminonicotinic acid ethyl ester (2.4 g) was suspended in dry toluene (50 ml). To the stirred suspension, 2,4,6-trifluorophenylacetyl chloride (3.0 g) in dry toluene (20 ml) was added. The resulting suspension was heated to reflux for 8 hours. The reaction mixture was cooled to ambient temperature, diluted with diethyl ether (100 ml), washed with water and brine, and the organic layer was dried over magnesium sulphate. The solvent was evaporated to give 2-[2-(2,4,6-trifluorophenyl)-acetylamino]-nicotinic acid ethyl ester as a yellow solid (4.5 g, 93%).

後処理

  1. temperatureThe resulting suspension was heated
  2. temperatureto reflux for 8 hours
  3. washwashed with water and brine
  4. dry with materialthe organic layer was dried over magnesium sulphate
  5. customThe solvent was evaporated

出典と根拠

ORDレコード
ord-809b9c4f66de4e5d932ec0565894e101
出典データセット
uspto-grants-2011_05
特許番号
US07947679B2

関連ノート

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