Nitrogen → 6-(6-Bromo-[1,2,4]triazolo[4,3-a]pyridin-3-ylthio)-3-(4-methylpiperazin-1-yl)quinoline

Participants

Reaction Conditions

Reaction Steps

A solution of Intermediate I (138 mg, 0.599 mmol), Intermediate Q14 (150 mg, 0.4 mmol), Pd2(dba)3 (36.6 mg, 0.04 mmol), xantphos (46.2 mg, 0.08 mmol) and DIPEA (0.14 ml, 0.799 mmol) in DMF (6 ml) was bubbled by N2 for 10 min, and then heated at 100° C. for 4 hours in oil bath. The reaction mixture was quenched with water and extracted with EtOAc for three times. The combined extract was washed with brine and dried over anhydrous Na2SO4. Solvent was evaporated and the residue was purified by silica gel chromatography to afford the title compound (0.08 g, 44% yield). LCMS (method A): [M+H]+=455/457, tR=1.7 min.

Provenance & Evidence