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2-Amino-5-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]thiophene-3-carboxamide → 5-[2,6-Difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-2-({6-methyl-5-[(methylsulfonyl)amino]pyridin-2-yl}amino)thiophene-3-carboxamide

HRID 386028
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HRID 386028 반응식
[NH2:1][C:2]1[S:3][C:4]([C:10]2[C:15]([F:16])=[CH:14][C:13]([C:17]([OH:20])([CH3:19])[CH3:18])=[CH:12][C:11]=2[F:21])=[CH:5][C:6]=1[C:7]([NH2:9])=[O:8].Cl[C:23]1[N:28]=[C:27]([CH3:29])[C:26]([N:30](S(C)(=O)=O)[S:31]([CH3:34])(=[O:33])=[O:32])=[CH:25][CH:24]=1>>[F:16][C:15]1[CH:14]=[C:13]([C:17]([OH:20])([CH3:18])[CH3:19])[CH:12]=[C:11]([F:21])[C:10]=1[C:4]1[S:3][C:2]([NH:1][C:23]2[CH:24]=[CH:25][C:26]([NH:30][S:31]([CH3:34])(=[O:32])=[O:33])=[C:27]([CH3:29])[N:28]=2)=[C:6]([C:7]([NH2:9])=[O:8])[CH:5]=1
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참가 물질

3

반응물 2

HCID 595256192-Amino-5-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]thiophene-3-carboxamideHCID 59526403N-(6-Chloro-2-methylpyridin-3-yl)-N-(methylsulfonyl)methanesulfonamide

생성물 1

HCID 595257465-[2,6-Difluoro-4-(1-hydroxy-1-methylethyl)phenyl]-2-({6-methyl-5-[(methylsulfonyl)amino]pyridin-2-yl}amino)thiophene-3-carboxamide

실험 절차

The title compounds were prepared in one pot as described in Example 1 using 2-amino-5-[2,6-difluoro-4-(1-hydroxy-1-methylethyl)phenyl]thiophene-3-carboxamide (150 mg, 0.48 mmol) and N-(6-chloro-2-methylpyridin-3-yl)-N(methylsulfonyl)methanesulfonamide (143 mg, 0.48 mmol) as starting materials. Mono and bis methylsulfonyl compounds were separated by column chromatography.

후처리

  1. customMono and bis methylsulfonyl compounds were separated by column chromatography

출처 및 근거

ORD 기록
ord-994c067532fc4635a67d2bcbe2a231b0
출처 데이터셋
uspto-grants-2013_02
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08367706B2

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