Triethylamine → 3-[3-(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-ureido]-propionic Acid Methyl Ester

HRID 11629

반응식

HRID 11629 반응식
[N+](C1C=CC(O[C:11](=[O:39])[NH:12][C:13]2[CH:18]=[C:17]([Cl:19])[CH:16]=[CH:15][C:14]=2[O:20][CH2:21][C:22]([N:24]2[CH2:29][CH2:28][N:27]([CH2:30][C:31]3[CH:36]=[CH:35][C:34]([F:37])=[CH:33][CH:32]=3)[CH2:26][C@H:25]2[CH3:38])=[O:23])=CC=1)([O-])=O.Cl.[CH3:41][O:42][C:43](=[O:47])[CH2:44][CH2:45][NH2:46].C(N(CC)CC)C>CO>[CH3:41][O:42][C:43](=[O:47])[CH2:44][CH2:45][NH:46][C:11]([NH:12][C:13]1[CH:18]=[C:17]([Cl:19])[CH:16]=[CH:15][C:14]=1[O:20][CH2:21][C:22]([N:24]1[CH2:29][CH2:28][N:27]([CH2:30][C:31]2[CH:36]=[CH:35][C:34]([F:37])=[CH:33][CH:32]=2)[CH2:26][C@H:25]1[CH3:38])=[O:23])=[O:39]

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 2734767Methyl 3-aminopropanoate hydrochlorideHCID 69655875(5-Chloro-2-(2-[4-(4-Fluoro-Benzyl)-(2R)-2-Methyl-Piperazin-1-Yl]-2-Oxo-Ethoxy}-Phenyl)-Carbamic Acid 4-Nitro-Phenyl Ester

생성물 1

HCID 696553713-[3-(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-ureido]-propionic Acid Methyl Ester수율 80%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

To a solution of (5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-carbamic acid 4-nitro-phenyl ester (0.10 g, 0.18 mmol) in methanol was added β-alanine methyl ester hydrochloride (0.038 g, 0.27 mmol) and triethylamine (0.038 mL, 0.27 mmol). The reaction was stirred at ambient temperature overnight. The reaction was concentrated and purified via chromatography on silica gel to give the title compound (0.075 g).

후처리

  1. concentrationThe reaction was concentrated
  2. custompurified via chromatography on silica gel

출처 및 근거

ORD 기록
ord-7f71fd0844e740eab34efa62eff663d6
출처 데이터셋
uspto-grants-2006_08
특허 번호
US07098212B2

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