1-tert-Butyl-5-methyl-1H-pyrazole-3-carbonyl chloride → HCID 86610441, 화합물

HRID 641009노트

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HRID 641009 반응식
[C:1]([N:5]1[C:9]([CH3:10])=[CH:8][C:7]([C:11](Cl)=[O:12])=[N:6]1)([CH3:4])([CH3:3])[CH3:2].[NH2:14][C:15]1[CH:16]=[C:17]([CH:30]=[CH:31][CH:32]=1)[C:18]([C:20]1[CH:28]=[C:27]2[C:23]([CH2:24][C:25](=[O:29])[NH:26]2)=[CH:22][CH:21]=1)=[O:19]>C1COCC1>[O:29]=[C:25]1[CH2:24][C:23]2[C:27](=[CH:28][C:20]([C:18]([C:17]3[CH:16]=[C:15]([NH:14][C:11]([C:7]4[CH:8]=[C:9]([CH3:10])[N:5]([C:1]([CH3:4])([CH3:3])[CH3:2])[N:6]=4)=[O:12])[CH:32]=[CH:31][CH:30]=3)=[O:19])=[CH:21][CH:22]=2)[NH:26]1

참가 물질

4

반응물 2

HCID 27356831-tert-Butyl-5-methyl-1H-pyrazole-3-carbonyl chlorideHCID 592564786-(3-Amino-benzoyl)-1,3-dihydro-indol-2-one

생성물 1

HCID 86610441HCID 86610441, 화합물수율 48%

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매2회

실험 절차

A dry flask was charged with 1-tert-Butyl-5-methyl-1H-pyrazole-3-carbonyl chloride (0.207 g, 1.032 mmol) and THF (10 mL). 6-(3-Amino-benzoyl)-1,3-dihydro-indol-2-one (as prepared in Example 40, 0.260 g, 1.03 mmol) was added to the THF solution of the acid chloride, and the mixture was allowed to reflux overnight. The reaction mixture was then allowed to cool to room temperature and subsequently vacuum filtered. The solid was washed with 0° C. THF (˜5 mL) and collected to afford the 1-tert-Butyl-5-methyl-1H-pyrazole-3-carboxylic acid [3-(2-oxo-2,3-dihydro-1H-indole-6-carbonyl)-phenyl]-amide as a solid (0.206 g, 0.490 mmol, 48%).

후처리

  1. temperatureto reflux overnight
  2. filtrationsubsequently vacuum filtered
  3. washThe solid was washed with 0° C
  4. customTHF (˜5 mL) and collected

출처 및 근거

ORD 기록
ord-94dc31ed6ef643b3b5208662f578e037
출처 데이터셋
uspto-grants-2010_04
특허 번호
US07692005B2

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