反应详情

温度

50 °C

An oven-dried flask was charged with 8.64 g (1-Chloro-6-methoxy-isoquinolin-3-yl)-(5-methyl-1H-pyrazol-3-yl)-amine, 0.54 g Pd(OAc)2, 1.2 g dppp, 0.3 g Pd(PPh3)4, 24 g Cs2CO3 in the solution of 200 mL i-PrOH and 200 mL DMF, then evacuated and filled with CO (4 bar) three cycles. The mixture was shaken at r.t 2 h, at 50° C. 2 h, then 90° C. overnight. After reaction completed, the solvent was removed, and the residue was dissolved in ethyl acetate, washed with water, dried with Na2SO4. After removal of solvent, the residue was purified by the column chromatography on solica gel to give 8.2 g of 6-Methoxy-3-(5-methyl-1H-pyrazol-3-ylamino)-isoquinoline-1-carboxylic acid isopropyl ester.

1. customevacuated
2. additionfilled with CO (4 bar) three cycles
3. custom2 h
4. custom90° C. overnight
5. customAfter reaction
6. customthe solvent was removed
7. dissolutionthe residue was dissolved in ethyl acetate
8. washwashed with water
9. dry with materialdried with Na2SO4
10. customAfter removal of solvent
11. customthe residue was purified by the column chromatography on solica gel