4-(Trifluoromethyl)pyridine-2-carboxylic acid → 4-trifluoromethyl-pyridine-2-carboxylic acid {(3RS,4SR)-4-(3,4-dichloro-phenyl)-1-[1-(1-methyl-cyclopropanecarbonyl)-piperidine-4-carbonyl]-pyrrolidin-3-yl}-methyl-amide

HRID 1951147ノート

反応式

HRID 1951147 の反応式
[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]([F:42])([F:41])[C:32]1[CH:37]=[CH:36][N:35]=[C:34]([C:38]([OH:40])=O)[CH:33]=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:38]([C:34]2[CH:33]=[C:32]([C:31]([F:30])([F:42])[F:41])[CH:37]=[CH:36][N:35]=2)=[O:40])[CH:5]=[CH:6][C:7]=1[Cl:8]

参加物

3

反応物 2

HCID 120251644-(Trifluoromethyl)pyridine-2-carboxylic acidHCID 67025815[(3SR,4RS)-3-(3,4-Dichloro-phenyl)-4-methylamino-pyrrolidin-1-yl]-[1-(1-methyl-cyclopropanecarbonyl)-piperidin-4-yl]-methanone

生成物 1

HCID 670256964-trifluoromethyl-pyridine-2-carboxylic acid {(3RS,4SR)-4-(3,4-dichloro-phenyl)-1-[1-(1-methyl-cyclopropanecarbonyl)-piperidine-4-carbonyl]-pyrrolidin-3-yl}-methyl-amide

実験手順

In analogy to the procedure described for the synthesis of example 97, the title compound 4-trifluoromethyl-pyridine-2-carboxylic acid {(3RS,4SR)-4-(3,4-dichloro-phenyl)-1-[1-(1-methyl-cyclopropanecarbonyl)-piperidine-4-carbonyl]-pyrrolidin-3-yl}-methyl-amide 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-(trifluoromethyl)pyridine-2-carboxylic acid instead of 4-chloro-3-(trifluoromethyl)benzoic acid and was obtained as a light brown foam. MS m/e: 611.2 [M]+.

後処理

  1. customIn analogy to the procedure described for the synthesis of example 97
  2. customwas obtained as a light brown foam

出典と根拠

ORDレコード
ord-44604128054d420b9884794f77e316a7
出典データセット
uspto-grants-2013_03
特許番号
US08404679B2

反応ノート

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