Tetrahydrofuran → N-(3,3,3-Trifluoro-propyl)-2-[4-trifluoromethyl-piperidinyl]-4-methylamino-5-amino-benzoic acid amide

HRID 1189697ノート

反応式

HRID 1189697 の反応式
[F:1][C:2]([F:30])([F:29])[CH2:3][CH2:4][NH:5][C:6](=[O:28])[C:7]1[CH:12]=[C:11]([N+:13]([O-])=O)[C:10]([NH:16][CH3:17])=[CH:9][C:8]=1[N:18]1[CH2:23][CH2:22][CH:21]([C:24]([F:27])([F:26])[F:25])[CH2:20][CH2:19]1.C1COCC1>[Pd].CO>[F:30][C:2]([F:1])([F:29])[CH2:3][CH2:4][NH:5][C:6](=[O:28])[C:7]1[CH:12]=[C:11]([NH2:13])[C:10]([NH:16][CH3:17])=[CH:9][C:8]=1[N:18]1[CH2:19][CH2:20][CH:21]([C:24]([F:27])([F:26])[F:25])[CH2:22][CH2:23]1

参加物

5

反応物 2

HCID 8028TetrahydrofuranHCID 86666489HCID 86666489、化合物

生成物 1

HCID 86666490N-(3,3,3-Trifluoro-propyl)-2-[4-trifluoromethyl-piperidinyl]-4-methylamino-5-amino-benzoic acid amide

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 887Methanol溶媒

実験手順

A mixture of N-(3,3,3-trifluoro-propyl)-2-[4-trifluoromethyl-piperidinyl]-4-methylamino-5-nitro-benzoic acid amide (2.5 g, 5.7 mmol), Pd/C (200 mg), THF (10 mL) and MeOH (100 mL) is stirred for 2 h under 3 bar H2-atmosphere. The mixture is filtered, and the filtrate is concentrated. Yield: 2.3 g. HPLC Rt=1.25 min (method A). MS m/z: 413 [M+H]+.

後処理

  1. filtrationThe mixture is filtered
  2. concentrationthe filtrate is concentrated

出典と根拠

ORDレコード
ord-338ece83c5464bebb7fd94fc1e4b8418
出典データセット
uspto-grants-2014_03
特許番号
US08674113B2

反応ノート

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