2-chloro-N-(5-methyl-1H-pyrazol-3-yl)-5-(trifluoromethyl)pyrimidin-4-amine → N2-(2,5-dimethyl-4-(piperidin-4-yl)phenyl)-N4-(5-methyl-1H-pyrazol-3-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine

HRID 1897724ノート

反応式

HRID 1897724 の反応式
Cl[C:2]1[N:7]=[C:6]([NH:8][C:9]2[CH:13]=[C:12]([CH3:14])[NH:11][N:10]=2)[C:5]([C:15]([F:18])([F:17])[F:16])=[CH:4][N:3]=1.C(OC([N:26]1[CH2:31][CH2:30][CH:29]([C:32]2[CH:37]=[C:36]([CH3:38])[C:35]([NH2:39])=[CH:34][C:33]=2[CH3:40])[CH2:28][CH2:27]1)=O)(C)(C)C>Cl.CC(O)C>[CH3:38][C:36]1[CH:37]=[C:32]([CH:29]2[CH2:28][CH2:27][NH:26][CH2:31][CH2:30]2)[C:33]([CH3:40])=[CH:34][C:35]=1[NH:39][C:2]1[N:7]=[C:6]([NH:8][C:9]2[CH:13]=[C:12]([CH3:14])[NH:11][N:10]=2)[C:5]([C:15]([F:18])([F:17])[F:16])=[CH:4][N:3]=1

参加物

5

反応物 2

HCID 582551692-chloro-N-(5-methyl-1H-pyrazol-3-yl)-5-(trifluoromethyl)pyrimidin-4-amineHCID 67155205Tert-butyl-4-(4-amino-2,5-dimethylphenyl)piperidine-1-carboxylate

生成物 1

HCID 58254965N2-(2,5-dimethyl-4-(piperidin-4-yl)phenyl)-N4-(5-methyl-1H-pyrazol-3-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine

試薬・触媒・溶媒 2

HCID 313Hydrochloric Acid触媒HCID 3776Isopropanol溶媒

反応条件

温度
150 °C

実験手順

A mixture of 2-chloro-N-(5-methyl-1H-pyrazol-3-yl)-5-(trifluoromethyl)pyrimidin-4-amine (513.0 mg, 0.9 mmol), tert-butyl-4-(4-amino-2,5-dimethylphenyl)piperidine-1-carboxylate (282.7 mg, 0.9 mmol), and concentrated aqueous HCl (10 drops) in i-PrOH (12 mL) was heated at 150° C. in a microwave reactor for 30 min. The crude product was purified by RP-HPLC to afford N2-(2,5-dimethyl-4-(piperidin-4-yl)phenyl)-N4-(5-methyl-1H-pyrazol-3-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine; ESMS m/z 446.2 (M+H+).

後処理

  1. customThe crude product was purified by RP-HPLC

出典と根拠

ORDレコード
ord-fa4d2cea410f426f863a6b7008b0c140
出典データセット
uspto-grants-2013_08
特許番号
US08519129B2

反応ノート

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