Pyridine → (5-Chloro-2-(2-[4-(4-Fluoro-Benzyl)-(2R)-2-Methyl-Piperazin-1-Yl]-2-Oxo-Ethoxy}-Phenyl)-Carbamic Acid 4-Nitro-Phenyl Ester

HRID 11628

반응식

HRID 11628 반응식
[NH2:1][C:2]1[CH:26]=[C:25]([Cl:27])[CH:24]=[CH:23][C:3]=1[O:4][CH2:5][C:6]([N:8]1[CH2:13][CH2:12][N:11]([CH2:14][C:15]2[CH:20]=[CH:19][C:18]([F:21])=[CH:17][CH:16]=2)[CH2:10][C@H:9]1[CH3:22])=[O:7].N1C=CC=CC=1.Cl[C:35]([O:37][C:38]1[CH:43]=[CH:42][C:41]([N+:44]([O-:46])=[O:45])=[CH:40][CH:39]=1)=[O:36]>ClCCl>[N+:44]([C:41]1[CH:40]=[CH:39][C:38]([O:37][C:35](=[O:36])[NH:1][C:2]2[CH:26]=[C:25]([Cl:27])[CH:24]=[CH:23][C:3]=2[O:4][CH2:5][C:6]([N:8]2[CH2:13][CH2:12][N:11]([CH2:14][C:15]3[CH:20]=[CH:19][C:18]([F:21])=[CH:17][CH:16]=3)[CH2:10][C@H:9]2[CH3:22])=[O:7])=[CH:43][CH:42]=1)([O-:46])=[O:45]

참가 물질

5

반응물 3

HCID 1049PyridineHCID 821294-Nitrophenyl chloroformateHCID 206109862-(2-Amino-4-chloro-phenoxy)-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone

생성물 1

HCID 69655875(5-Chloro-2-(2-[4-(4-Fluoro-Benzyl)-(2R)-2-Methyl-Piperazin-1-Yl]-2-Oxo-Ethoxy}-Phenyl)-Carbamic Acid 4-Nitro-Phenyl Ester수율 99.7%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

To a solution of 2-(2-amino-4-chloro-phenoxy)-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone (0.14 g, 0.36 mmol) in dichloromethane (5 mL) was added pyridine (0.032 mL, 0.39 mmol) and 4-nitrophenyl chloroformate (0.079 g, 0.39 mmol). The reaction was stirred at ambient temperature for one hour and concentrated in vacuo to give the title compound (0.20 g).

후처리

  1. concentrationconcentrated in vacuo

출처 및 근거

ORD 기록
ord-cfd19eb5d2bc4c8bbfbf484c02e6d7bb
출처 데이터셋
uspto-grants-2006_08
특허 번호
US07098212B2

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