2-Methyl-5-(trifluoromethoxy)benzoic acid → 5-(3,4-Dimethoxyphenyl)-4,4-dimethyl-2-(1-{[2-methyl-5-(trifluoromethoxy)phenyl]carbonyl}piperidin-4-yl)-2,4-dihydro-3H-pyrazol-3-one

HRID 1914180노트

반응식

HRID 1914180 반응식
Cl.[CH3:2][O:3][C:4]1[CH:5]=[C:6]([C:12]2[C:13]([CH3:25])([CH3:24])[C:14](=[O:23])[N:15]([CH:17]3[CH2:22][CH2:21][NH:20][CH2:19][CH2:18]3)[N:16]=2)[CH:7]=[CH:8][C:9]=1[O:10][CH3:11].[CH3:26][C:27]1[CH:35]=[CH:34][C:33]([O:36][C:37]([F:40])([F:39])[F:38])=[CH:32][C:28]=1[C:29](O)=[O:30]>>[CH3:2][O:3][C:4]1[CH:5]=[C:6]([C:12]2[C:13]([CH3:25])([CH3:24])[C:14](=[O:23])[N:15]([CH:17]3[CH2:22][CH2:21][N:20]([C:29]([C:28]4[CH:32]=[C:33]([O:36][C:37]([F:38])([F:39])[F:40])[CH:34]=[CH:35][C:27]=4[CH3:26])=[O:30])[CH2:19][CH2:18]3)[N:16]=2)[CH:7]=[CH:8][C:9]=1[O:10][CH3:11]

참가 물질

3

반응물 2

HCID 588390582-Methyl-5-(trifluoromethoxy)benzoic acid2회HCID 666164065-(3,4-dimethoxyphenyl)-4,4-dimethyl-2-piperidin-4-yl-2,4-dihydro-3H-pyrazol-3-one hydrochloride2회

생성물 1

HCID 673630665-(3,4-Dimethoxyphenyl)-4,4-dimethyl-2-(1-{[2-methyl-5-(trifluoromethoxy)phenyl]carbonyl}piperidin-4-yl)-2,4-dihydro-3H-pyrazol-3-one

실험 절차

The title compound is prepared analogously as described for GP2-WU2 using 5-(3,4-dimethoxyphenyl)-4,4-dimethyl-2-piperidin-4-yl-2,4-dihydro-3H-pyrazol-3-one (compound B1) and 2-methyl-5-(trifluoromethoxy)benzoic acid (compound F5) as starting compounds. The crude product is purified by chromatography (amino phase silica gel and DCM) and by crystallization from DCM and diethyl ether to yield the title compound.

후처리

  1. customThe title compound is prepared analogously
  2. customThe crude product is purified by chromatography (amino phase silica gel and DCM) and by crystallization from DCM and diethyl ether

출처 및 근거

ORD 기록
ord-4521f219fda4432e9c1d310d1c8a6168
출처 데이터셋
uspto-grants-2013_12
특허 번호
US08609848B2

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