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Diethyl Pyrocarbonate → 3-(4-tert-Butylphenyl)propynoic Acid N-[1-(3-fluoro-4-methanesulfonylamino-5-vinylphenyl)ethyl]amide

HRID 2358394
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HRID 2358394 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]([C:28]#[C:29][C:30](O)=[O:31])=[CH:24][CH:23]=1)([CH3:21])([CH3:20])[CH3:19].CCOC(OC(OCC)=O)=O>CN(C=O)C>[F:17][C:6]1[CH:5]=[C:4]([CH:2]([NH:1][C:30](=[O:31])[C:29]#[C:28][C:25]2[CH:26]=[CH:27][C:22]([C:18]([CH3:20])([CH3:19])[CH3:21])=[CH:23][CH:24]=2)[CH3:3])[CH:9]=[C:8]([CH:10]=[CH2:11])[C:7]=1[NH:12][S:13]([CH3:16])(=[O:15])=[O:14]
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

5

반응물 3

HCID 3051Diethyl PyrocarbonateHCID 113447013-(4-tert-butylphenyl)prop-2-ynoic AcidHCID 68455310N-[4-(1-Aminoethyl)-2-fluoro-6-vinylphenyl]methanesulfonamide

생성물 1

HCID 118525783-(4-tert-Butylphenyl)propynoic Acid N-[1-(3-fluoro-4-methanesulfonylamino-5-vinylphenyl)ethyl]amide수율 95.09%

시약·촉매·용매 1

HCID 6228
Dimethylformamide
용매

실험 절차

N-[4-(1-Amino-ethyl)-2-fluoro-6-vinylphenyl]methanesulfonamide (0.03 mmol, 10.0 mg), (4-tert-butylphenyl)propynoic acid (step 2 of Example 11, 0.03 mmol, 6.52 mg), DEPC (0.03 mmol, 5.46 μl), and TEA (0.06 mmol, 8.36 μl) were added into DMF. The mixture was stirred for 12 hr. The reaction mixture was purified according to Example 12 to give a title product (11.3 mg, 95.09%).

후처리

  1. customThe reaction mixture was purified

출처 및 근거

ORD 기록
ord-9a48bb2f719142fbabf17f3da134e125
출처 데이터셋
uspto-grants-2010_07
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07763657B2

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