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Diethyl Pyrocarbonate → (R)-3-(4-tert-Butylphenyl)-N-[1-(3-fluoro-4-methanesulfonylamino-5-vinylphenyl)ethyl]acrylamide

HRID 2358404
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HRID 2358404 반응식
[NH2:1][CH:2]([C:4]1[CH:9]=[C:8]([CH:10]=[CH2:11])[C:7]([NH:12][S:13]([CH3:16])(=[O:15])=[O:14])=[C:6]([F:17])[CH:5]=1)[CH3:3].[C:18]([C:22]1[CH:27]=[CH:26][C:25]([CH:28]=[CH:29][C:30](O)=[O:31])=[C:24](NCCC(C)C)[CH:23]=1)([CH3:21])([CH3:20])[CH3:19].CCOC(OC(OCC)=O)=O>CN(C=O)C>[C:18]([C:22]1[CH:23]=[CH:24][C:25]([CH:28]=[CH:29][C:30]([NH:1][C@@H:2]([C:4]2[CH:9]=[C:8]([CH:10]=[CH2:11])[C:7]([NH:12][S:13]([CH3:16])(=[O:15])=[O:14])=[C:6]([F:17])[CH:5]=2)[CH3:3])=[O:31])=[CH:26][CH:27]=1)([CH3:21])([CH3:19])[CH3:20]
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참가 물질

5

반응물 3

HCID 3051Diethyl PyrocarbonateHCID 68453138HCID 68453138, 화합물HCID 68455310N-[4-(1-Aminoethyl)-2-fluoro-6-vinylphenyl]methanesulfonamide

생성물 1

HCID 68457488(R)-3-(4-tert-Butylphenyl)-N-[1-(3-fluoro-4-methanesulfonylamino-5-vinylphenyl)ethyl]acrylamide수율 100%

시약·촉매·용매 1

HCID 6228Dimethylformamide
용매

실험 절차

N-[4-(1-Aminoethyl)-2-fluoro-6-vinylphenyl]methanesulfonamide (0.7 mmol, 25.3 mg), 3-[4-tert-butyl-2-(3-methylbutylamino)phenyl]acrylic acid (0.7 mmol, 15.27 mg), DEPC (0.08 mmol, 12.75 μl), and TEA (0.14 mmol, 19.51 μl) were added in DMF. The reaction mixture was stirred for 12 hrs. The reaction mixture was purified according to similar procedure of Example 21 to yield title product (36.1 mg, 100.0%).

후처리

  1. customThe reaction mixture was purified

출처 및 근거

ORD 기록
ord-a1ffcc37e93841cb9a97e24b160ce650
출처 데이터셋
uspto-grants-2010_07
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07763657B2

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