1-tert-Butyl-5-methyl-1H-pyrazole-3-carbonyl chloride → HCID 86610441、化合物

HRID 641009ノート

反応式

HRID 641009 の反応式
[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

参加物

4

反応物 2

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

生成物 1

HCID 86610441HCID 86610441、化合物収率 48%

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒2 回

実験手順

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%).

後処理

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

出典と根拠

ORDレコード
ord-94dc31ed6ef643b3b5208662f578e037
出典データセット
uspto-grants-2010_04
特許番号
US07692005B2

反応ノート

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