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Trifluoroacetic acid → 2-[(R)-4-(2-fluoro-4-trifluoromethoxy-benzenesulfonyl)-3-(4-propyl-benzylcarbamoyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid

HRID 908602
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HRID 908602 반응식
C([O:5][C:6]([C:8]1[S:12][C:11]([N:13]2[CH2:18][CH2:17][N:16]([S:19]([C:22]3[CH:27]=[CH:26][C:25]([O:28][C:29]([F:32])([F:31])[F:30])=[CH:24][C:23]=3[F:33])(=[O:21])=[O:20])[C@@H:15]([C:34](=[O:46])[NH:35][CH2:36][C:37]3[CH:42]=[CH:41][C:40]([CH2:43][CH2:44][CH3:45])=[CH:39][CH:38]=3)[CH2:14]2)=[N:10][C:9]=1[CH3:47])=[O:7])(C)(C)C.FC(F)(F)C(O)=O>C(Cl)(Cl)Cl>[F:33][C:23]1[CH:24]=[C:25]([O:28][C:29]([F:30])([F:31])[F:32])[CH:26]=[CH:27][C:22]=1[S:19]([N:16]1[CH2:17][CH2:18][N:13]([C:11]2[S:12][C:8]([C:6]([OH:7])=[O:5])=[C:9]([CH3:47])[N:10]=2)[CH2:14][C@@H:15]1[C:34](=[O:46])[NH:35][CH2:36][C:37]1[CH:38]=[CH:39][C:40]([CH2:43][CH2:44][CH3:45])=[CH:41][CH:42]=1)(=[O:20])=[O:21]
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 597037082-[(R)-4-(2-fluoro-4-trifluoromethoxy-benzenesulfonyl)-3-(4-propyl-benzylcarbamoyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid tert-butyl ester

생성물 1

HCID 597037632-[(R)-4-(2-fluoro-4-trifluoromethoxy-benzenesulfonyl)-3-(4-propyl-benzylcarbamoyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid수율 82.9%

시약·촉매·용매 1

HCID 6212
Chloroform
용매

실험 절차

To a solution of the compound (59 mg) obtained in Step 7 in chloroform (0.3 ml) was added, with stirring at room temperature, trifluoroacetic acid (0.3 ml). After stirring at room temperature for 7 hr, the reaction mixture was concentrated under reduced pressure, toluene was added to the residue, and the mixture was concentrated again under reduced pressure. The residue was purified by column chromatography (ethyl acetate:n-hexane=1:2-10% methanol/chloroform) to give the title compound (45 mg).

후처리

  1. stirringAfter stirring at room temperature for 7 hr
  2. concentrationthe reaction mixture was concentrated under reduced pressure, toluene
  3. additionwas added to the residue
  4. concentrationthe mixture was concentrated again under reduced pressure
  5. customThe residue was purified by column chromatography (ethyl acetate:n-hexane=1:2-10% methanol/chloroform)

출처 및 근거

ORD 기록
ord-e24294657e804f4c9476d735636ceaf3
출처 데이터셋
uspto-grants-2011_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08017612B2

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