Triethylamine → 2,2,2-Trifluoro-N-(5-((4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)methyl)-2,3-dihydro-1H-inden-1-yl)acetamide

HRID 43025

反応式

HRID 43025 の反応式
[NH2:1][CH:2]1[C:10]2[C:5](=[CH:6][C:7]([CH2:11][N:12]3[CH:16]=[C:15]([CH2:17][OH:18])[C:14]([C:19]([F:22])([F:21])[F:20])=[N:13]3)=[CH:8][CH:9]=2)[CH2:4][CH2:3]1.C(N(CC)CC)C.[F:30][C:31]([F:38])([F:37])[C:32](OCC)=[O:33]>C(Cl)Cl>[F:30][C:31]([F:38])([F:37])[C:32]([NH:1][CH:2]1[C:10]2[C:5](=[CH:6][C:7]([CH2:11][N:12]3[CH:16]=[C:15]([CH2:17][OH:18])[C:14]([C:19]([F:22])([F:21])[F:20])=[N:13]3)=[CH:8][CH:9]=2)[CH2:4][CH2:3]1)=[O:33]

参加物

5

反応物 3

HCID 8471TriethylamineHCID 9794Ethyl trifluoroacetateHCID 58230802(1-((1-Amino-2,3-dihydro-1H-inden-5-yl)methyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)methanol

生成物 1

HCID 445557322,2,2-Trifluoro-N-(5-((4-(hydroxymethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)methyl)-2,3-dihydro-1H-inden-1-yl)acetamide

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a solution of (1-((1-amino-2,3-dihydro-1H-inden-5-yl)methyl)-3-(trifluoromethyl)-1H-pyrazol-4-yl)methanol (0.199 mmol, 62.1 mg) and triethylamine (0.399 mmol, 0.056 mL, 40.4 mg) in DCM (1.2 mL) was added a solution of ethyl 2,2,2-trifluoroacetate (0.199 mmol, 0.024 mL, 28.3 mg) and the whole stirred at room temperature for 60 h. The reaction mixture was concentrated under reduced pressure and the residue purified by RP-HPLC to give a clear film (30.0 mg, 0.074 mmol, 36.9%). MS (ESI): m/z [M+H]+ 408.0.

後処理

  1. concentrationThe reaction mixture was concentrated under reduced pressure
  2. customthe residue purified by RP-HPLC
  3. customto give a clear film (30.0 mg, 0.074 mmol, 36.9%)

出典と根拠

ORDレコード
ord-6e1b65ccf55a4352b3757c81b5b6f475
出典データセット
uspto-grants-2013_09
特許番号
US08536214B2

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