Ethanol → (3-{3-[Cyclopropyl(methyl)amino]-1,2,4-oxadiazol-5-yl}-5-[4-(trifluoromethyl)phenyl]piperidin-1-yl)(morpholin-4-yl)methanone

HRID 661266ノート

反応式

HRID 661266 の反応式
Cl[C:2]1[N:6]=[C:5]([CH:7]2[CH2:12][CH:11]([C:13]3[CH:18]=[CH:17][C:16]([C:19]([F:22])([F:21])[F:20])=[CH:15][CH:14]=3)[CH2:10][N:9]([C:23]([N:25]3[CH2:30][CH2:29][O:28][CH2:27][CH2:26]3)=[O:24])[CH2:8]2)[O:4][N:3]=1.[CH:31]1([CH2:34][NH2:35])[CH2:33]C1.[CH2:36](O)C>>[CH:34]1([N:35]([CH3:36])[C:2]2[N:6]=[C:5]([CH:7]3[CH2:12][CH:11]([C:13]4[CH:18]=[CH:17][C:16]([C:19]([F:22])([F:21])[F:20])=[CH:15][CH:14]=4)[CH2:10][N:9]([C:23]([N:25]4[CH2:30][CH2:29][O:28][CH2:27][CH2:26]4)=[O:24])[CH2:8]3)[O:4][N:3]=2)[CH2:31][CH2:33]1

参加物

4

反応条件

温度
90 °C

実験手順

To a solution of 109 mg (0.245 mmol) of the oxadiazole from Example 23A in 2.0 ml of ethanol were added 523 mg (7.35 mmol) of cyclopropylmethylamine, and then the reaction mixture was stirred in the microwave at 90° C. for 12 h. The solvent was removed under reduced pressure and the crude product was purified by means of preparative HPLC. Yield: 42.0 mg (36% of theory)

後処理

  1. customThe solvent was removed under reduced pressure
  2. customthe crude product was purified by means of preparative HPLC

出典と根拠

ORDレコード
ord-214eb9ad2b2c4edfa21a8ce7efedf63f
出典データセット
uspto-grants-2011_12
特許番号
US08084469B2

反応ノート

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