3-Difluoromethyl-phenylboronic acid → (R)-5-(3-Difluoromethyl-phenyl)-1-(2-methoxy-1-methyl-ethyl)-6-methyl-4-oxo-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide

HRID 524355

反応式

HRID 524355 の反応式
[CH3:1][S:2]([C:5]1[CH:28]=[CH:27][C:8]([CH2:9][NH:10][C:11]([C:13]2[C:18](=[O:19])[C:17](Br)=[C:16]([CH3:21])[N:15]([C@H:22]([CH3:26])[CH2:23][O:24][CH3:25])[CH:14]=2)=[O:12])=[CH:7][CH:6]=1)(=[O:4])=[O:3].[F:29][CH:30]([F:40])[C:31]1[CH:32]=[C:33](B(O)O)[CH:34]=[CH:35][CH:36]=1>>[CH3:1][S:2]([C:5]1[CH:28]=[CH:27][C:8]([CH2:9][NH:10][C:11]([C:13]2[C:18](=[O:19])[C:17]([C:35]3[CH:34]=[CH:33][CH:32]=[C:31]([CH:30]([F:40])[F:29])[CH:36]=3)=[C:16]([CH3:21])[N:15]([C@H:22]([CH3:26])[CH2:23][O:24][CH3:25])[CH:14]=2)=[O:12])=[CH:7][CH:6]=1)(=[O:4])=[O:3]

参加物

3

反応物 2

HCID 447172443-Difluoromethyl-phenylboronic acidHCID 89978794(R)-5-Bromo-1-(2-methoxy-1-methyl-ethyl)-6-methyl-4-oxo-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide

生成物 1

HCID 89978697(R)-5-(3-Difluoromethyl-phenyl)-1-(2-methoxy-1-methyl-ethyl)-6-methyl-4-oxo-1,4-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide

実験手順

Example 44 is prepared following the procedure for Example 24.1, substituting preparation 24 with preparation 43c and replacing 3-(trifluoromethyl)phenylboronic acid with 3-(difluoromethyl)phenylboronic acid. ESI mass spectrum: [M+H]+=519; Retention time HPLC: 0.97 min (Z018_S04).

後処理

  1. customExample 44 is prepared
  2. custompreparation 24
  3. custom0.97 min (Z018_S04)

出典と根拠

ORDレコード
ord-fca7e6965e9f4e1ba99e5104a0a37065
出典データセット
uspto-grants-2016_05
特許番号
US09340507B2

関連ノート

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