2-(4-(Methylsulfonyl)piperazin-1-yl)ethanol → 2-Bromo-3-(3,5-difluorophenyl)-6-(2-(4-(methylsulfonyl)piperazin-1-yl)ethoxy)-1H-inden-1-one

HRID 331309노트

반응식

HRID 331309 반응식
[Br:1][C:2]1[C:3](=[O:20])[C:4]2[C:9]([C:10]=1[C:11]1[CH:16]=[C:15]([F:17])[CH:14]=[C:13]([F:18])[CH:12]=1)=[CH:8][CH:7]=[C:6]([OH:19])[CH:5]=2.BrC1C(=O)C2C(C=1C1C=CC=CC=1)=CC=C(O)C=2.[CH3:39][S:40]([N:43]1[CH2:48][CH2:47][N:46]([CH2:49][CH2:50]O)[CH2:45][CH2:44]1)(=[O:42])=[O:41]>>[Br:1][C:2]1[C:3](=[O:20])[C:4]2[C:9]([C:10]=1[C:11]1[CH:12]=[C:13]([F:18])[CH:14]=[C:15]([F:17])[CH:16]=1)=[CH:8][CH:7]=[C:6]([O:19][CH2:50][CH2:49][N:46]1[CH2:47][CH2:48][N:43]([S:40]([CH3:39])(=[O:41])=[O:42])[CH2:44][CH2:45]1)[CH:5]=2

참가 물질

4

반응물 3

HCID 27624262-(4-(Methylsulfonyl)piperazin-1-yl)ethanolHCID 703061762-bromo-6-hydroxy-3-phenyl-1H-inden-1-oneHCID 703160432-Bromo-3-(3,5-difluorophenyl)-6-hydroxy-1H-inden-1-one

생성물 1

HCID 703100942-Bromo-3-(3,5-difluorophenyl)-6-(2-(4-(methylsulfonyl)piperazin-1-yl)ethoxy)-1H-inden-1-one수율 99%

실험 절차

The procedure of Step 6 of Example 1 was repeated except for using 2-bromo-3-(3,5-difluorophenyl)-6-hydroxy-1H-inden-1-one obtained in Step 5 of Example 36 as a starting material instead of 2-bromo-6-hydroxy-3-phenyl-1H-inden-1-one, 2-(4-(methylsulfonyl)piperazin-1-yl)ethanol instead of 4-(2-hydroxyethyl)morpholine, being stirred for 4 d, and being purified by silica gel column chromatography (CH2Cl2/EtOAc=1:2) to obtain the title compound (99%)

후처리

  1. custombeing purified by silica gel column chromatography (CH2Cl2/EtOAc=1:2)

출처 및 근거

ORD 기록
ord-e79b368b6fbe46a6bc7a9c1935b0651e
출처 데이터셋
uspto-grants-2014_11
특허 번호
US08877747B2

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