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2-[(R)-3-[(6-isopropyl-pyridin-3-ylmethyl)-carbamoyl]-4-(4-trifluoromethoxy-benzenesulfonyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid tert-butyl ester → 2-[(R)-3-[(6-isopropyl-pyridin-3-ylmethyl)-carbamoyl]-4-(4-trifluoromethoxy-benzenesulfonyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid

HRID 908596
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HRID 908596 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][CH:23]=3)(=[O:21])=[O:20])[C@@H:15]([C:33](=[O:45])[NH:34][CH2:35][C:36]3[CH:37]=[N:38][C:39]([CH:42]([CH3:44])[CH3:43])=[CH:40][CH:41]=3)[CH2:14]2)=[N:10][C:9]=1[CH3:46])=[O:7])(C)(C)C>FC(F)(F)C(O)=O>[CH:42]([C:39]1[N:38]=[CH:37][C:36]([CH2:35][NH:34][C:33]([C@@H:15]2[N:16]([S:19]([C:22]3[CH:23]=[CH:24][C:25]([O:28][C:29]([F:32])([F:30])[F:31])=[CH:26][CH:27]=3)(=[O:21])=[O:20])[CH2:17][CH2:18][N:13]([C:11]3[S:12][C:8]([C:6]([OH:7])=[O:5])=[C:9]([CH3:46])[N:10]=3)[CH2:14]2)=[O:45])=[CH:41][CH:40]=1)([CH3:44])[CH3:43]
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참가 물질

3

반응물 1

HCID 597038392-[(R)-3-[(6-isopropyl-pyridin-3-ylmethyl)-carbamoyl]-4-(4-trifluoromethoxy-benzenesulfonyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid tert-butyl ester

생성물 1

HCID 250560612-[(R)-3-[(6-isopropyl-pyridin-3-ylmethyl)-carbamoyl]-4-(4-trifluoromethoxy-benzenesulfonyl)-piperazin-1-yl]-4-methyl-thiazole-5-carboxylic acid수율 85.2%

시약·촉매·용매 1

HCID 6422Trifluoroacetic acid용매

실험 절차

A solution of the compound (55 mg) obtained in Step 7 in trifluoroacetic acid (330 μl) was stirred at room temperature for 1 hr. The reaction mixture was concentrated under reduced pressure, chloroform was added to the residue, and the mixture was concentrated again under reduced pressure. The residue was purified by thin layer chromatography (methanol:chloroform=1:10) to give the title compound (43 mg).

후처리

  1. concentrationThe reaction mixture was concentrated under reduced pressure, chloroform
  2. additionwas added to the residue
  3. concentrationthe mixture was concentrated again under reduced pressure
  4. customThe residue was purified by thin layer chromatography (methanol:chloroform=1:10)

출처 및 근거

ORD 기록
ord-b097ca330fa94f18bb7472267097d45b
출처 데이터셋
uspto-grants-2011_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08017612B2

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