Trifluoroacetic acid → HCID 178461788、化合物

HRID 1011823ノート

反応式

HRID 1011823 の反応式
FC(F)(F)C(O)=O.[N:8]1([C:12]([C:14]2[N:15]=[CH:16][C:17]([O:20][C:21]3[CH:22]=[C:23]([C:35]([NH:37][C:38]4[CH:42]=[CH:41][N:40](C(OC(C)(C)C)=O)[N:39]=4)=[O:36])[CH:24]=[C:25]([O:27][C@@H:28]([CH3:34])[CH2:29][O:30][CH:31]([F:33])[F:32])[CH:26]=3)=[N:18][CH:19]=2)=[O:13])[CH2:11][CH2:10][CH2:9]1>C(Cl)Cl>[N:8]1([C:12]([C:14]2[N:15]=[CH:16][C:17]([O:20][C:21]3[CH:22]=[C:23]([CH:24]=[C:25]([O:27][C@@H:28]([CH3:34])[CH2:29][O:30][CH:31]([F:33])[F:32])[CH:26]=3)[C:35]([NH:37][C:38]3[CH:42]=[CH:41][NH:40][N:39]=3)=[O:36])=[N:18][CH:19]=2)=[O:13])[CH2:9][CH2:10][CH2:11]1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 591271291,1-dimethylethyl 3-({[3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-({(1S)-2-[(difluoromethyl)oxy]-1-methylethyl}oxy)phenyl]carbonyl}amino)-1H-pyrazole-1-carboxylate

生成物 1

HCID 178461788HCID 178461788、化合物収率 112%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

Trifluoroacetic acid (2 mL) was added to a solution of 1,1-dimethylethyl 3-({[3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-({(1S)-2-[(difluoromethyl)oxy]-1-methylethyl}oxy)phenyl]carbonyl}amino)-1H-pyrazole-1-carboxylate (115 mg, 0.17 mmol) in DCM (16 mL) and stirred at RT for 2 hours. The solvent was removed in vacuo, DCM (20 mL) added and the mixture washed with water (20 mL), a saturated solution of sodium bicarbonate (20 mL), brine (20 mL), dried (MgSO4), filtered and reduced in vacuo to give the desired compound as a white foam (93 mg).

後処理

  1. customThe solvent was removed in vacuo, DCM (20 mL)
  2. additionadded
  3. washthe mixture washed with water (20 mL)
  4. dry with materiala saturated solution of sodium bicarbonate (20 mL), brine (20 mL), dried (MgSO4)
  5. filtrationfiltered

出典と根拠

ORDレコード
ord-fed96540577a449180f9e2c57fe9d833
出典データセット
uspto-grants-2011_07
特許番号
US07977328B2

反応ノート

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