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3-(2-(Isopropoxycarbonylamino-methyl)-4-{2-[5-methyl-2-(4-nitro-phenyl)-oxazol-4-yl]-ethoxy}-phenyl)-propionic acid tert-butyl ester → 3-[4-{2-[2-(4-Amino-phenyl)-5-methyl-oxazol-4-yl]-ethoxy}-2-(isopropoxycarbonylamino-methyl)-phenyl]-propionic acid tert-butyl ester

HRID 1181072
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인쇄 미리보기

반응식

HRID 1181072 반응식
[C:1]([O:5][C:6](=[O:41])[CH2:7][CH2:8][C:9]1[CH:14]=[CH:13][C:12]([O:15][CH2:16][CH2:17][C:18]2[N:19]=[C:20]([C:24]3[CH:29]=[CH:28][C:27]([N+:30]([O-])=O)=[CH:26][CH:25]=3)[O:21][C:22]=2[CH3:23])=[CH:11][C:10]=1[CH2:33][NH:34][C:35]([O:37][CH:38]([CH3:40])[CH3:39])=[O:36])([CH3:4])([CH3:3])[CH3:2]>CCOC(C)=O.[Pd]>[C:1]([O:5][C:6](=[O:41])[CH2:7][CH2:8][C:9]1[CH:14]=[CH:13][C:12]([O:15][CH2:16][CH2:17][C:18]2[N:19]=[C:20]([C:24]3[CH:25]=[CH:26][C:27]([NH2:30])=[CH:28][CH:29]=3)[O:21][C:22]=2[CH3:23])=[CH:11][C:10]=1[CH2:33][NH:34][C:35]([O:37][CH:38]([CH3:39])[CH3:40])=[O:36])([CH3:4])([CH3:3])[CH3:2]
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

4

반응물 1

HCID 589793583-(2-(Isopropoxycarbonylamino-methyl)-4-{2-[5-methyl-2-(4-nitro-phenyl)-oxazol-4-yl]-ethoxy}-phenyl)-propionic acid tert-butyl ester

생성물 1

HCID 589790083-[4-{2-[2-(4-Amino-phenyl)-5-methyl-oxazol-4-yl]-ethoxy}-2-(isopropoxycarbonylamino-methyl)-phenyl]-propionic acid tert-butyl ester수율 100%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 8857Ethyl Acetate용매

실험 절차

A mixture of 3-(2-(isopropoxycarbonylamino-methyl)-4-{2-[5-methyl-2-(4-nitro-phenyl)-oxazol-4-yl]-ethoxy}-phenyl)-propionic acid tert-butyl ester (207 mg, 0.365 mmol) and 10% Pd—C (27 mg) in EtOAc (20 mL) was stirred under H2 (1 atm) for 18 h. The reaction mixture was filtered through Celite and concentrated (75° C.) to give the title compound as a colorless oil (196 mg, 100%): MS (ESI) m/z 538 (M+H)+.

후처리

  1. filtrationThe reaction mixture was filtered through Celite
  2. concentrationconcentrated (75° C.)

출처 및 근거

ORD 기록
ord-7277c6b79ba6411cbefa8664f00c5aa8
출처 데이터셋
uspto-grants-2007_10
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07282501B2

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