Pyridine → HCID 178449817、化合物

HRID 1053623ノート

反応式

HRID 1053623 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]([C:7]([N:9]([CH2:19][CH:20]2[CH2:23][CH2:22][CH2:21]2)[CH2:10][C:11]2[CH:16]=[CH:15][C:14]([OH:17])=[CH:13][C:12]=2[F:18])=[O:8])[NH:5]C=1.[C:24]([NH:31][C@:32]([C:36]([OH:38])=O)([CH3:35])[CH2:33][CH3:34])([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25].C1CCC([N:45]=C=NC2CCCCC2)CC1.N1C=CC=CC=1>C(OCC)(=O)C>[C:24]([NH:31][C@@:32]([CH3:35])([CH2:33][CH3:34])[C:36]([O:17][C:14]1[CH:15]=[CH:16][C:11]([CH2:10][N:9]([CH2:19][CH:20]2[CH2:21][CH2:22][CH2:23]2)[C:7]([C:4]2[NH:5][N:45]=[C:2]([Cl:1])[CH:3]=2)=[O:8])=[C:12]([F:18])[CH:13]=1)=[O:38])([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25]

参加物

6

反応物 4

HCID 1049PyridineHCID 10868DicyclohexylcarbodiimideHCID 14284791(R)-2-((tert-Butoxycarbonyl)amino)-2-methylbutanoic acidHCID 901023224-chloro-N-(cyclobutylmethyl)-N-(2-fluoro-4-hydroxybenzyl)-1H-pyrrole-2-carboxamide

生成物 1

HCID 178449817HCID 178449817、化合物収率 0%

試薬・触媒・溶媒 1

HCID 8857Ethyl Acetate溶媒

実験手順

To a solution of 4-chloro-N-(cyclobutylmethyl)-N-(2-fluoro-4-hydroxybenzyl)-1H-pyrrole-2-carboxamide (0.040 g, 0.118 mmol) in 3 mL ethyl acetate was added Boc-iso-Valine (0.026 g, 0.118 mmol), DCC (0.037 g, 0.178 mmol) and pyridine 0.5 mL. The reaction mixture was added at r.t. for overnight. After removal of all the solvent, the residue was purified by chromatography. (0-30% methanol/DCM) (S)-4-((3-chloro-N-(cyclobutylmethyl)-1H-pyrazole-5-carboxamido)methyl)-3-fluorophenyl 2-(Boc-amino)-2-methylbutanoate was obtained (0.030 g, 0.056 mmol, 47% yield).

後処理

  1. additionThe reaction mixture was added at r.t. for overnight
  2. customAfter removal of all the solvent
  3. customthe residue was purified by chromatography

出典と根拠

ORDレコード
ord-32d28061defe445d994651e37e6336f0
出典データセット
uspto-grants-2016_07
特許番号
US09394257B2

反応ノート

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