Pyridine → 3,4-dichloro-N-[1-[6-chloro-4-[(E)-N-hydroxy-C-methylcarbonimidoyl]-2-pyridinyl]piperidin-4-yl]-5-methyl-1H-pyrrole-2-carboxamide

HRID 2233940ノート

反応式

HRID 2233940 の反応式
[C:1]([C:4]1[CH:9]=[C:8]([Cl:10])[N:7]=[C:6]([N:11]2[CH2:16][CH2:15][CH:14]([NH:17][C:18]([C:20]3[NH:21][C:22]([CH3:27])=[C:23]([Cl:26])[C:24]=3[Cl:25])=[O:19])[CH2:13][CH2:12]2)[CH:5]=1)(=O)[CH3:2].N1C=CC=CC=1.Cl.[NH2:35][OH:36]>CCO>[Cl:25][C:24]1[C:23]([Cl:26])=[C:22]([CH3:27])[NH:21][C:20]=1[C:18]([NH:17][CH:14]1[CH2:15][CH2:16][N:11]([C:6]2[CH:5]=[C:4](/[C:1](=[N:35]/[OH:36])/[CH3:2])[CH:9]=[C:8]([Cl:10])[N:7]=2)[CH2:12][CH2:13]1)=[O:19]

参加物

5

反応物 3

HCID 1049PyridineHCID 443297Hydroxyamine hydrochlorideHCID 86608290N-[1-(4-Acetyl-6-chloro-2-pyridinyl)-4-piperidinyl]-3,4-dichloro-5-methyl-1H-pyrrole-2-carboxamide

生成物 1

HCID 1363325053,4-dichloro-N-[1-[6-chloro-4-[(E)-N-hydroxy-C-methylcarbonimidoyl]-2-pyridinyl]piperidin-4-yl]-5-methyl-1H-pyrrole-2-carboxamide

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

N-[1-(4-Acetyl-6-chloropyridin-2-yl)piperidin-4-yl]-3,4-dichloro-5-methyl-1H-pyrrole-2-carboxamide (Example 115) (49 mg, 0.114 mmol) was dissolved in EtOH (2 ml). Pyridine (74 μl, 0.913 mmol) was added followed by hydroxylamine hydrochloride (63.4 mg, 0.913 mmol). The mixture was stirred at room temperature overnight. The product was purified by semi-prep reverse phase HPLC eluting with CH3CN/H2O (0.1% TFA). (28 mg).

後処理

  1. customThe product was purified by semi-prep reverse phase HPLC
  2. washeluting with CH3CN/H2O (0.1% TFA)

出典と根拠

ORDレコード
ord-89c109adcfb543afa89abb601fc4d102
出典データセット
uspto-grants-2010_05
特許番号
US07709503B2

反応ノート

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