Trifluoroacetic acid → (2-Fluoro-3-methoxy-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)phenyl)(morpholino)methanone

HRID 1804684ノート

反応式

HRID 1804684 の反応式
[NH2:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]([N:10]2[CH2:15][CH2:14][O:13][CH2:12][CH2:11]2)=[O:9])=[C:4]([F:16])[C:3]=1[O:17][CH3:18].Cl[C:20]1[N:25]=[C:24]([NH:26][CH3:27])[C:23]([C:28]([F:31])([F:30])[F:29])=[CH:22][N:21]=1.C(O)(C(F)(F)F)=O>COCCO>[F:16][C:4]1[C:3]([O:17][CH3:18])=[C:2]([NH:1][C:20]2[N:25]=[C:24]([NH:26][CH3:27])[C:23]([C:28]([F:31])([F:29])[F:30])=[CH:22][N:21]=2)[CH:7]=[CH:6][C:5]=1[C:8]([N:10]1[CH2:11][CH2:12][O:13][CH2:14][CH2:15]1)=[O:9]

参加物

5

反応物 3

HCID 6422Trifluoroacetic acidHCID 210775872-Chloro-N-methyl-5-(trifluoromethyl)pyrimidin-4-amineHCID 58539264(4-Amino-2-fluoro-3-methoxyphenyl)(morpholino)methanone

生成物 1

HCID 58539237(2-Fluoro-3-methoxy-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)phenyl)(morpholino)methanone

試薬・触媒・溶媒 1

HCID 80192-Methoxyethanol溶媒

反応条件

温度
95 °C

実験手順

A mixture of (4-amino-2-fluoro-3-methoxyphenyl)(morpholino)methanone (0.18 g, 0.72 mmol) and 2-chloro-N-methyl-5-(trifluoromethyl)pyrimidin-4-amine (0.10 g, 0.47 mmol) in a solution of 2-methoxyethanol (2 mL) and TFA (0.055 mL) was stirred at 95° C. for 2 hours. The reaction was concentrated and purified by reverse phase HPLC to give the title compound. Additional compounds made using the above procedure are shown in Table 6 below.

後処理

  1. concentrationThe reaction was concentrated
  2. custompurified by reverse phase HPLC

出典と根拠

ORDレコード
ord-10007359dad04cf4b8cb3b1a73f3616a
出典データセット
uspto-grants-2013_01
特許番号
US08354420B2

反応ノート

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