Ethanol → (3-{3-[Cyclopropyl(methyl)amino]-1,2,4-oxadiazol-5-yl}-5-[4-(trifluoromethyl)phenyl]piperidin-1-yl)(morpholin-4-yl)methanone
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
反応物 3
生成物 1
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
- customThe solvent was removed under reduced pressure
- 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
読み込み中…