4-Fluorobenzoyl chloride → N-{(3RS,4SR)-4-(3,4-Dichloro-phenyl)-1-[1-(1-methyl-cyclopropanecarbonyl)-piperidine-4-carbonyl]-pyrrolidin-3-yl}-4-fluoro-N-methyl-benzamide

HRID 1951096노트

반응식

HRID 1951096 반응식
[Cl:1][C:2]1[CH:3]=[C:4]([CH:9]2[CH:13]([NH:14][CH3:15])[CH2:12][N:11]([C:16]([CH:18]3[CH2:23][CH2:22][N:21]([C:24]([C:26]4([CH3:29])[CH2:28][CH2:27]4)=[O:25])[CH2:20][CH2:19]3)=[O:17])[CH2:10]2)[CH:5]=[CH:6][C:7]=1[Cl:8].[F:30][C:31]1[CH:39]=[CH:38][C:34]([C:35](Cl)=[O:36])=[CH:33][CH:32]=1>>[Cl:1][C:2]1[CH:3]=[C:4]([CH:9]2[CH2:10][N:11]([C:16]([CH:18]3[CH2:19][CH2:20][N:21]([C:24]([C:26]4([CH3:29])[CH2:27][CH2:28]4)=[O:25])[CH2:22][CH2:23]3)=[O:17])[CH2:12][CH:13]2[N:14]([CH3:15])[C:35](=[O:36])[C:34]2[CH:38]=[CH:39][C:31]([F:30])=[CH:32][CH:33]=2)[CH:5]=[CH:6][C:7]=1[Cl:8]

참가 물질

3

반응물 2

HCID 678794-Fluorobenzoyl chlorideHCID 67025815[(3SR,4RS)-3-(3,4-Dichloro-phenyl)-4-methylamino-pyrrolidin-1-yl]-[1-(1-methyl-cyclopropanecarbonyl)-piperidin-4-yl]-methanone

생성물 1

HCID 67025592N-{(3RS,4SR)-4-(3,4-Dichloro-phenyl)-1-[1-(1-methyl-cyclopropanecarbonyl)-piperidine-4-carbonyl]-pyrrolidin-3-yl}-4-fluoro-N-methyl-benzamide

실험 절차

In analogy to the procedure described for the synthesis of example 96 (step e), the title compound N-{(3RS,4SR)-4-(3,4-dichloro-phenyl)-1-[1-(1-methyl-cyclopropanecarbonyl)-piperidine-4-carbonyl]-pyrrolidin-3-yl}-4-fluoro-N-methyl-benzamide was prepared from {4-[(3SR,4RS)-3-(3,4-dichloro-phenyl)-4-methylamino-pyrrolidine-1-carbonyl]-piperidin-1-yl}-(1-methyl-cyclopropyl)-methanone using 4-fluorobenzoyl chloride instead of 4-methoxy-3-(trifluoromethyl)benzoyl chloride and was obtained as a light brown foam. MS m/e: 560.1 [M]+.

후처리

  1. customIn analogy to the procedure described for the synthesis of example 96 (step e)
  2. customwas obtained as a light brown foam

출처 및 근거

ORD 기록
ord-87fb259792eb4bbdb04ab80504c74880
출처 데이터셋
uspto-grants-2013_03
특허 번호
US08404679B2

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