反应 #554674

反应方程式

5-Bromopyrazin-2-amine

K3PO4

(4-isopropylsulfonylphenyl)boronic acid

→

sub-title compound

收率 80.7%

5-(4-(Isopropylsulfonyl)phenyl)pyrazin-2-amine

收率 80.7%

溶剂

EtOAc

water

MeCN

Water

反应条件

后处理

1. 1
   workup.ADDITIONwas added
2. 2
   温度The reaction mixture was cooled to ambient temperature
3. 3
   其他The layers were separated
4. 4
   萃取the aqueous layer extracted with EtOAc (×3)
5. 5
   干燥The combined organic layers were dried (MgSO4)
6. 6
   过滤filtered
7. 7
   浓缩concentrated in vacuo
8. 8
   其他The residue was triturated from DCM
9. 9
   其他isolated by filtration

实验过程

5-Bromopyrazin-2-amine (5 g, 28.74 mmol), (4-isopropylsulfonylphenyl)boronic acid (7.866 g, 34.49 mmol) and K3PO4 (12.20 g, 57.48 mmol) were combined in MeCN (100 mL)/Water (25 mL) and Pd[P(tBu)3]2 (734.4 mg, 1.437 mmol) was added. The reaction was heated at 60° C. for 1 hour. The reaction mixture was cooled to ambient temperature and diluted with EtOAc and water. The layers were separated and the aqueous layer extracted with EtOAc (×3). The combined organic layers were dried (MgSO4), filtered and concentrated in vacuo. The residue was triturated from DCM and isolated by filtration to give the sub-title compound as an orange solid (6.43 g, 76% Yield). 1H NMR (400.0 MHz, DMSO) δ 1.17 (d, 6H), 3.43 (sept, 1H), 6.86 (s, 2H), 7.87 (d, 2H), 8.00 (s, 1H), 8.20 (d, 2H) and 8.67 (s, 1H) ppm; MS (ES+) 278.2.

来源