Tert-butyl 4-[2-cyano-4-(trifluoromethyl)phenyl]piperazine-1-carboxylate → 4-(2-Aminomethyl-4-trifluoromethyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester

HRID 1667537노트

반응식

HRID 1667537 반응식
[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][N:11]([C:14]2[CH:19]=[CH:18][C:17]([C:20]([F:23])([F:22])[F:21])=[CH:16][C:15]=2[C:24]#[N:25])[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[H][H]>N.CCO.[Ni]>[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][N:11]([C:14]2[CH:19]=[CH:18][C:17]([C:20]([F:21])([F:22])[F:23])=[CH:16][C:15]=2[CH2:24][NH2:25])[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:2])[CH3:3]

참가 물질

5

반응물 2

HCID 59793685Tert-butyl 4-[2-cyano-4-(trifluoromethyl)phenyl]piperazine-1-carboxylateHCID 178418361HCID 178418361, 화합물

생성물 1

HCID 674164364-(2-Aminomethyl-4-trifluoromethyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester수율 98.1%

시약·촉매·용매 2

HCID 935Nickel촉매HCID 22020343Ethanol, reaction products with ammonia, distn. residues용매

실험 절차

To a solution 4-(2-cyano-4-trifluoromethyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (150 mg, 0.42 mmol) in NH3/EtOH (2M, 10 mL) was added Raney Nickel (3 mL slurry in water). The atmosphere was exchanged with hydrogen via balloon and the mixture was allowed to stir for 30 min. After this time the mixture was filtered through celite and concentrated to yield the title compound (148 mg). m/z (M+1) 360.23.

후처리

  1. filtrationAfter this time the mixture was filtered through celite and
  2. concentrationconcentrated

출처 및 근거

ORD 기록
ord-aa41e98393b74a2f86512878b1c764cc
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08044041B2

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