Trifluoroacetic acid → HCID 178474033、化合物

HRID 537070ノート

反応式

HRID 537070 の反応式
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH2:8][N:9]2[CH2:13][CH2:12][CH2:11][CH2:10]2)=[CH:4][C:3]=1[C:14]1[O:18][C:17]([C:19]2[C:24]([CH3:25])=[CH:23][N:22]=[C:21]([NH:26][C:27](=[O:29])[CH3:28])[CH:20]=2)=[CH:16][C:15]=1[C:30]1[N:34]=[CH:33][N:32](COCC[Si](C)(C)C)[N:31]=1.C(O)(C(F)(F)F)=O>C(Cl)Cl>[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([CH2:8][N:9]2[CH2:10][CH2:11][CH2:12][CH2:13]2)=[CH:4][C:3]=1[C:14]1[O:18][C:17]([C:19]2[C:24]([CH3:25])=[CH:23][N:22]=[C:21]([NH:26][C:27](=[O:29])[CH3:28])[CH:20]=2)=[CH:16][C:15]=1[C:30]1[NH:34][CH:33]=[N:32][N:31]=1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 66749388N-(4-{5-[2-chloro-5-(pyrrolidin-1-ylmethyl)phenyl]-4-(1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-1,2,4-triazol-3-yl)-2-furyl}-5-methylpyridin-2-yl)acetamide

生成物 1

HCID 178474033HCID 178474033、化合物収率 86.3%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a solution of N-(4-{5-[2-chloro-5-(pyrrolidin-1-ylmethyl)phenyl]-4-(1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-1,2,4-triazol-3-yl)-2-furyl}-5-methylpyridin-2-yl)acetamide (0.20 g, 0.34 mmol) in DCM (5 mL) was added TFA (2 mL). The mixture was allowed to stir at rt overnight. The mixture was concentrated and the residue was purified by column chromatography to give N-(4-{5-[2-chloro-5-(pyrrolidin-1-ylmethyl)phenyl]-4-(4H-1,2,4-triazol-3-yl)-2-furyl}-5-methylpyridin-2-yl)acetamide (0.14 g, 81%). LCMS (FA): m/z=477.6 (M+H).

後処理

  1. concentrationThe mixture was concentrated
  2. customthe residue was purified by column chromatography

出典と根拠

ORDレコード
ord-4fd36a0f84424a78a9c6a8e6425807b2
出典データセット
uspto-grants-2014_10
特許番号
US08859768B2

反応ノート

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