Triethylamine → Ethyl 3-[3-([2-(diethoxyphosphoryl)propanoyl]aminomethyl)-4-methoxyphenyl]-2-isopropoxypropionate

HRID 1816595

반응식

HRID 1816595 반응식
[CH2:1]([O:3][P:4]([CH:9]([CH3:13])[C:10]([OH:12])=O)([O:6][CH2:7][CH3:8])=[O:5])[CH3:2].[NH2:14][CH2:15][C:16]1[CH:17]=[C:18]([CH2:24][CH:25]([O:31][CH:32]([CH3:34])[CH3:33])[C:26]([O:28][CH2:29][CH3:30])=[O:27])[CH:19]=[CH:20][C:21]=1[O:22][CH3:23].C(P(=O)(OCC)OCC)#N.C(N(CC)CC)C>CN(C)C=O.C(OCC)(=O)C>[CH2:7]([O:6][P:4]([CH:9]([CH3:13])[C:10]([NH:14][CH2:15][C:16]1[CH:17]=[C:18]([CH2:24][CH:25]([O:31][CH:32]([CH3:33])[CH3:34])[C:26]([O:28][CH2:29][CH3:30])=[O:27])[CH:19]=[CH:20][C:21]=1[O:22][CH3:23])=[O:12])([O:3][CH2:1][CH3:2])=[O:5])[CH3:8]

참가 물질

7

반응물 4

HCID 8471TriethylamineHCID 76257Diethyl cyanophosphonateHCID 118059462-diethylphosphonopropionic acidHCID 22493983Ethyl 3-[3-(aminomethyl)-4-methoxyphenyl]-2-isopropoxypropanoate

생성물 1

HCID 22494119Ethyl 3-[3-([2-(diethoxyphosphoryl)propanoyl]aminomethyl)-4-methoxyphenyl]-2-isopropoxypropionate수율 87.8%

시약·촉매·용매 2

HCID 6228Dimethylformamide용매HCID 8857Ethyl Acetate용매

실험 절차

643 mg of 2-diethylphosphonopropionic acid and 973 mg of ethyl 3-[3-(aminomethyl)-4-methoxyphenyl]-2-isopropoxypropionate were dissolved in 10 ml N,N-dimethylformamide, and 470 μl diethyl cyanophosphonate and 1.07 ml triethylamine were successively added thereto. The mixture was stirred overnight at room temperature, and the reaction mixture was diluted with ethyl acetate. The organic layer was washed with water and brine, dried over anhydrous magnesium sulfate and the solvent was evaporated, to give 1.310 g of ethyl 3-[3-([2-(diethoxyphosphoryl)propanoyl]aminomethyl)-4-methoxyphenyl]-2-isopropoxypropionate.

후처리

  1. washThe organic layer was washed with water and brine
  2. dry with materialdried over anhydrous magnesium sulfate
  3. customthe solvent was evaporated

출처 및 근거

ORD 기록
ord-008f4e5077ed4761a53b45479caa79fa
출처 데이터셋
uspto-grants-2005_04
특허 번호
US06884821B1

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