Methyl morpholine oxide → 2-Acetyl-N-(3,4-difluorobenzyl)-6-isopropoxy-1-(pyridin-2-ylmethyl)-1H-indole-3-carboxamide

HRID 40108ノート

反応式

HRID 40108 の反応式
[F:1][C:2]1[CH:3]=[C:4]([CH:32]=[CH:33][C:34]=1[F:35])[CH2:5][NH:6][C:7]([C:9]1[C:17]2[C:12](=[CH:13][C:14]([O:18][CH:19]([CH3:21])[CH3:20])=[CH:15][CH:16]=2)[N:11]([CH2:22][C:23]2[CH:28]=[CH:27][CH:26]=[CH:25][N:24]=2)[C:10]=1[CH:29]([OH:31])[CH3:30])=[O:8].C[N+]1([O-])CCOCC1>C(Cl)Cl.CCC[N+](CCC)(CCC)CCC.[O-][Ru](=O)(=O)=O>[C:29]([C:10]1[N:11]([CH2:22][C:23]2[CH:28]=[CH:27][CH:26]=[CH:25][N:24]=2)[C:12]2[C:17]([C:9]=1[C:7]([NH:6][CH2:5][C:4]1[CH:32]=[CH:33][C:34]([F:35])=[C:2]([F:1])[CH:3]=1)=[O:8])=[CH:16][CH:15]=[C:14]([O:18][CH:19]([CH3:21])[CH3:20])[CH:13]=2)(=[O:31])[CH3:30]

参加物

5

反応物 2

HCID 82029Methyl morpholine oxideHCID 59762339HCID 59762339、化合物2 回

生成物 1

HCID 597623482-Acetyl-N-(3,4-difluorobenzyl)-6-isopropoxy-1-(pyridin-2-ylmethyl)-1H-indole-3-carboxamide

試薬・触媒・溶媒 2

HCID 178419074HCID 178419074、化合物触媒HCID 6344Dichloromethane溶媒

実験手順

To a solution of N-(3,4-difluorobenzyl)-2-(1-hydroxyethyl)-6-isopropoxy-1-(pyridin-2-ylmethyl)-1H-indole-3-carboxamide (Compound 108, 8.0 mg, 0.017 mmol) in CH2Cl2 (1 ml) was added NMO (6.0 mg, 0.051 mmol) and TPAP (0.6 mg, 0.0017 mmol). The reaction was stirred at room temperature for 1 h and was purified directly by PTLC (75% EtOAc-hexanes) to yield the title compound.

後処理

  1. customwas purified directly by PTLC (75% EtOAc-hexanes)

出典と根拠

ORDレコード
ord-a62061fc31174a1087b623258c6d1993
出典データセット
uspto-grants-2013_09
特許番号
US08524917B2

反応ノート

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