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

HRID 550357

반응식

HRID 550357 반응식
[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]

참가 물질

5

반응물 2

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

생성물 1

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

시약·촉매·용매 2

HCID 1140Toluene용매2회HCID 3283Diethyl Ether용매

실험 절차

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%).

후처리

  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

출처 및 근거

ORD 기록
ord-809b9c4f66de4e5d932ec0565894e101
출처 데이터셋
uspto-grants-2011_05
특허 번호
US07947679B2

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