Potassium Carbonate → 1-(2-Chloro-3,6-difluorobenzyl)-8-methyl-7-[3-(morpholin-4-yl)phenyl]-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine

Participants

Reaction Steps

To a solution of 7-bromo-1-(2-chloro-3,6-difluorobenzyl)-8-methyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (0.048 g, 0.124 mmol) and 3-morpholinophenylboronic acid pinacol ester (0.035 g, 0.124 mmol) in DMF-H2O (9:1, 2 mL) was added PdCl2(PPh3)2 (0.0087 g, 0.0124 mmol) and K2CO3 (0.043 mg, 0.31 mmol). The resulting solution was subjected to microwave irradiation at 125° C. for 20 min. The solvent was filtered using a PTFE frit and then directly purified by prep HPLC using a gradient mixture of ACN—H2O— 0.1% TFA to yield the desired product (0.023 g 40%).

Provenance & Evidence