反应详情

As shown in step 9-iv of Scheme 9, A suspension of Compound 1030 (2.46 g, 8.745 mmol) in 6N aq. HCl (43 mL) was stirred at room temperature for 2 hours. The crude reaction mixture was neutralizes at ˜4° C. by the slow addition of 6N NaOH followed by the addition of 1N aq. K2CO3). The reaction was extracted with EtOAc (3×) and the combined organics dried (MgSO4), followed by concentration under reduced pressure to give 1-(5,6-dimethoxypyrazin-2-yl)piperidin-4-one as an off white semi solid (Compound 1031, 1.51 g, 73%), which was used in the next step without further purification: 1H NMR (CDCl3, 300 MHz) δ 7.33 (s, 1H), 4.07 (s, 3H), 4.04 (s, 3H), 3.86 (m, 4H), 2.62 (m, 4H) ppm.

1. customThe crude reaction mixture
2. customat ˜4° C.
3. extractionThe reaction was extracted with EtOAc (3×)
4. dry with materialthe combined organics dried (MgSO4)
5. concentrationfollowed by concentration under reduced pressure