2-Bromo-1-(thiophen-3-yl)ethan-1-one → 4-((Bis(3-fluorophenyl)methoxy)carbonyl)-1-methyl-1-(2-oxo-2-(thiophen-3-yl)ethyl)piperidinium bromide

HRID 1910517노트

반응식

HRID 1910517 반응식
[Br:1][CH2:2][C:3]([C:5]1[CH:9]=[CH:8][S:7][CH:6]=1)=[O:4].[CH3:10][N:11]1[CH2:16][CH2:15][CH:14]([C:17]([O:19][CH:20]([C:28]2[CH:33]=[CH:32][CH:31]=[C:30]([F:34])[CH:29]=2)[C:21]2[CH:26]=[CH:25][CH:24]=[C:23]([F:27])[CH:22]=2)=[O:18])[CH2:13][CH2:12]1>CCOC(C)=O>[Br-:1].[F:34][C:30]1[CH:29]=[C:28]([CH:20]([C:21]2[CH:26]=[CH:25][CH:24]=[C:23]([F:27])[CH:22]=2)[O:19][C:17]([CH:14]2[CH2:13][CH2:12][N+:11]([CH3:10])([CH2:2][C:3](=[O:4])[C:5]3[CH:9]=[CH:8][S:7][CH:6]=3)[CH2:16][CH2:15]2)=[O:18])[CH:33]=[CH:32][CH:31]=1

참가 물질

4

반응물 2

HCID 27763792-Bromo-1-(thiophen-3-yl)ethan-1-oneHCID 70925814Bis(3-fluorophenyl)methyl 1-methylpiperidine-4-carboxylate

생성물 1

HCID 866729504-((Bis(3-fluorophenyl)methoxy)carbonyl)-1-methyl-1-(2-oxo-2-(thiophen-3-yl)ethyl)piperidinium bromide수율 54.7%

시약·촉매·용매 1

HCID 8857Ethyl Acetate용매

실험 절차

2-Bromo-1-(thiophen-3-yl)ethanone (23.7 mg, 0.12 mmol) was added to a solution of bis(3-fluorophenyl)methyl 1-methylpiperidine-4-carboxylate (40 mg, 0.12 mmol, prepared as in example 40) in EtOAc (3 ml). The reaction was stirred at room temperature overnight. The solvent was evaporated, and the crude was purified by preparative HPLC (eluent: CH3CN/H2O) to obtain 4-((bis(3-fluorophenyl)methoxy)carbonyl)-1-methyl-1-(2-oxo-2-(thiophen-3-yl)ethyl)piperidinium bromide (36.1 mg).

후처리

  1. customThe solvent was evaporated
  2. customthe crude was purified by preparative HPLC (eluent: CH3CN/H2O)

출처 및 근거

ORD 기록
ord-b024410d0e2e44739b78fe8e56360f5f
출처 데이터셋
uspto-grants-2013_12
특허 번호
US08604015B2

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