反应详情

A solution of tert-butyl 4-(3-(4-(5-methylpyridin-2-ylamino)phenoxy)pyrazin-2-yl)piperidine-1-carboxylate (0.220 g, 0.434 mmol) in DCM (5 mL) was added 4M HCl in dioxane (2 mL). After stirring for 2 h at RT, diisopropylethylamine (0.525 mL, 3.01 mmol), 2-methoxyacetic acid (0.077 mL, 1.004 mmol), and HATU (0.305 g, 0.803 mmol) was added and the reaction mixture was stirred at RT in 2 h. Water was added and the mixture was extracted with DCM (3×), dried over Na2SO4, concentrated. The crude material was purified by reverse phase HPLC, then neutralized with saturated NaHCO3, extracted with DCM (3×), dried over Na2SO4, concentrated to give the title compound. MS (ESI, pos. ion) m/z: 434.2 (M+1). IC50 (uM) 0.000058.

1. stirringthe reaction mixture was stirred at RT in 2 h
2. extractionthe mixture was extracted with DCM (3×)
3. dry with materialdried over Na2SO4
4. concentrationconcentrated
5. customThe crude material was purified by reverse phase HPLC
6. extractionextracted with DCM (3×)
7. dry with materialdried over Na2SO4
8. concentrationconcentrated