反応式
Cl[C:2]1[C:7]([CH3:8])=[C:6]([C:9]2[O:10][CH:11]=[CH:12][CH:13]=2)[N:5]=[C:4]([NH2:14])[N:3]=1.[C:15](#[N:17])C>>[NH2:14][C:4]1[N:3]=[C:2]([C:15]#[N:17])[C:7]([CH3:8])=[C:6]([C:9]2[O:10][CH:11]=[CH:12][CH:13]=2)[N:5]=1参加物
3
反応条件
- 温度
- 140 °C
実験手順
A solution of 4-chloro-6-(2-furyl)-5-methylpyrimidine-2-amine (80 mg, 0.38 mmol) in acetonitrile (4 mL) was treated with polymer supported cyamide (0.636 mg, 1.91 mmol), stirred at 140° C. in the microwave for 30 min, filtered to remove the resin and the filter cake washed with acetonitrile. The filtrate was concentrated in vacuo to give the title compound (50 mg, 65%) as off-white solid; NMR δH (400 MHz, DMSO) 2.48 (3H, s), 6.75 (1H, dd, J 1.7, 3.5 Hz), 7.04 (2H br s), 7.28 (1H, dd, J 0.7, 3.5 Hz) and 8.00 (1H, dd, J 0.7, 1.7 Hz); M/Z 201 (M=H)+; HPLC 1.1 min. (50/80).
後処理
- filtrationfiltered
- customto remove the resin
- washthe filter cake washed with acetonitrile
- concentrationThe filtrate was concentrated in vacuo
出典と根拠
- ORDレコード
- ord-c74d9c1988604ab2acf5b2d783e0e5bb
- 出典データセット
- uspto-grants-2011_01
- 特許番号
- US07875600B2
関連ノート
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