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Trifluoroacetic acid → N-Cyclopropyl-3-fluoro-5-[2-(3-hydroxy-2,2-dimethylpropyl)-1-oxo-4-{[(8aR)-3-oxotetrahydro[1,3]oxazolo[3,4-a]pyrazin-7(1H)-yl]sulfonyl}-1,2-dihydroisoquinolin-6-yl]-4-methylbenzamide

HRID 906452
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인쇄 미리보기

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HRID 906452 반응식
[Si]([O:8][CH2:9][C:10]([CH3:56])([CH3:55])[CH2:11][N:12]1[CH:21]=[C:20]([S:22]([N:25]2[CH2:30][CH2:29][N:28]([C:31]([O:33]C(C)(C)C)=[O:32])[C@@H:27]([CH2:38]O)[CH2:26]2)(=[O:24])=[O:23])[C:19]2[C:14](=[CH:15][CH:16]=[C:17]([C:40]3[CH:45]=[C:44]([C:46](=[O:51])[NH:47][CH:48]4[CH2:50][CH2:49]4)[CH:43]=[C:42]([F:52])[C:41]=3[CH3:53])[CH:18]=2)[C:13]1=[O:54])(C(C)(C)C)(C)C.FC(F)(F)C(O)=O>C(Cl)Cl.C1(C)C=CC=CC=1>[CH:48]1([NH:47][C:46](=[O:51])[C:44]2[CH:45]=[C:40]([C:17]3[CH:18]=[C:19]4[C:14](=[CH:15][CH:16]=3)[C:13](=[O:54])[N:12]([CH2:11][C:10]([CH3:56])([CH3:55])[CH2:9][OH:8])[CH:21]=[C:20]4[S:22]([N:25]3[CH2:30][CH2:29][N:28]4[C:31](=[O:32])[O:33][CH2:38][C@H:27]4[CH2:26]3)(=[O:24])=[O:23])[C:41]([CH3:53])=[C:42]([F:52])[CH:43]=2)[CH2:49][CH2:50]1
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

5

반응물 2

HCID 6422Trifluoroacetic acidHCID 86640972tert-Butyl (2R)-4-({2-(3-{[tert-butyl(dimethyl)silyl]oxy}-2,2-dimethylpropyl)-6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-1-oxo-1,2-dihydroisoquinolin-4-yl}sulfonyl)-2-(hydroxymethyl)piperazine-1-carboxylate

생성물 1

HCID 67389817N-Cyclopropyl-3-fluoro-5-[2-(3-hydroxy-2,2-dimethylpropyl)-1-oxo-4-{[(8aR)-3-oxotetrahydro[1,3]oxazolo[3,4-a]pyrazin-7(1H)-yl]sulfonyl}-1,2-dihydroisoquinolin-6-yl]-4-methylbenzamide

시약·촉매·용매 2

HCID 1140Toluene용매
HCID 6344Dichloromethane용매

실험 절차

tert-Butyl (2R)-4-({2-(3-{[tert-butyl(dimethyl)silyl]oxy}-2,2-dimethylpropyl)-6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-1-oxo-1,2-dihydroisoquinolin-4-yl}sulfonyl)-2-(hydroxymethyl)piperazine-1-carboxylate (Example 49c, 0.537 g) was dissolved in DCM (10 mL) and treated with trifluoroacetic acid (3 mL). The reaction mixture was diluted with toluene (5 mL) and evaporated under reduced pressure.

후처리

  1. customevaporated under reduced pressure

출처 및 근거

ORD 기록
ord-f69bb622365f4cac85999e9dff74149d
출처 데이터셋
uspto-grants-2011_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08012980B2

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