1-ethyl-3-methyl-1H-pyrazol-4-amine → (1-Ethyl-3-methyl-1H-pyrazol-4-yl)-[2-(6-trifluoromethyl-pyridin-3-yl)-ethyl]-amine

HRID 1094392

반응식

HRID 1094392 반응식
[CH2:1]([N:3]1[CH:7]=[C:6]([NH2:8])[C:5]([CH3:9])=[N:4]1)[CH3:2].[F:10][C:11]([F:22])([F:21])[C:12]1[N:17]=[CH:16][C:15]([CH2:18][C:19]#N)=[CH:14][CH:13]=1>CO.[Pd]>[CH2:1]([N:3]1[CH:7]=[C:6]([NH:8][CH2:19][CH2:18][C:15]2[CH:16]=[N:17][C:12]([C:11]([F:22])([F:10])[F:21])=[CH:13][CH:14]=2)[C:5]([CH3:9])=[N:4]1)[CH3:2]

참가 물질

5

반응물 2

HCID 64853541-ethyl-3-methyl-1H-pyrazol-4-amineHCID 508511273-Pyridineacetonitrile, 6-(trifluoromethyl)-

생성물 1

HCID 58007521(1-Ethyl-3-methyl-1H-pyrazol-4-yl)-[2-(6-trifluoromethyl-pyridin-3-yl)-ethyl]-amine수율 13%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 887Methanol용매

실험 절차

A solution of 1-ethyl-3-methyl-1H-pyrazol-4-ylamine (1.345 g, 10.75 mmol, commercially available) and (6-trifluoromethyl-pyridin-3-yl)-acetonitrile (distilled 166-175° C./2 mb, 1.0 g, 5.4 mmol) in MeOH (10 mL) was treated with HCO2NH4 (1.694 g, 26.86 mmol) and 10% Pd/C (200 mg) and stirred at 80° for 1.5 h. Filtration, concentration and purification by HPLC afforded the title compound (0.213 g, 13%) as a light brown oil. MS m/e: 299.3 [M+H]+.

후처리

  1. filtrationFiltration, concentration and purification by HPLC

출처 및 근거

ORD 기록
ord-5c4b8b4faffd4ba9b1da5ef83f166845
출처 데이터셋
uspto-grants-2012_03
특허 번호
US08133909B2

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