3-Difluoromethyl-phenylboronic acid → 5-(3-Difluoromethyl-phenyl)-1-isopropyl-6-methyl-4-oxo-1,4-dihydro-pyridine-3-carboxylic acid (5-methanesulfonyl-thiophen-2-ylmethyl)-amide

HRID 524353

반응식

HRID 524353 반응식
[CH3:1][S:2]([C:5]1[S:9][C:8]([CH2:10][NH:11][C:12]([C:14]2[C:19](=[O:20])[C:18](Br)=[C:17]([CH3:22])[N:16]([CH:23]([CH3:25])[CH3:24])[CH:15]=2)=[O:13])=[CH:7][CH:6]=1)(=[O:4])=[O:3].[F:26][CH:27]([F:37])[C:28]1[CH:29]=[C:30](B(O)O)[CH:31]=[CH:32][CH:33]=1>>[CH3:1][S:2]([C:5]1[S:9][C:8]([CH2:10][NH:11][C:12]([C:14]2[C:19](=[O:20])[C:18]([C:32]3[CH:31]=[CH:30][CH:29]=[C:28]([CH:27]([F:37])[F:26])[CH:33]=3)=[C:17]([CH3:22])[N:16]([CH:23]([CH3:25])[CH3:24])[CH:15]=2)=[O:13])=[CH:7][CH:6]=1)(=[O:4])=[O:3]

참가 물질

3

반응물 2

HCID 447172443-Difluoromethyl-phenylboronic acidHCID 899828075-Bromo-1-isopropyl-6-methyl-4-oxo-1,4-dihydro-pyridine-3-carboxylic acid (5-methanesulfonyl-thiophen-2-ylmethyl)-amide

생성물 1

HCID 899828095-(3-Difluoromethyl-phenyl)-1-isopropyl-6-methyl-4-oxo-1,4-dihydro-pyridine-3-carboxylic acid (5-methanesulfonyl-thiophen-2-ylmethyl)-amide

실험 절차

Example 40 is prepared following the procedure for Example 24.1, substituting preparation 24 with preparation 39a and replacing 3-(trifluoromethyl)phenylboronic acid with 3-(difluoromethyl)phenylboronic acid. ESI mass spectrum: [M+H]+=495; Retention time HPLC: 0.82 min (Z011_S03).

후처리

  1. customExample 40 is prepared
  2. custompreparation 24

출처 및 근거

ORD 기록
ord-d807105bbafc409190552bf0eb805327
출처 데이터셋
uspto-grants-2016_05
특허 번호
US09340507B2

연결된 노트

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