反应详情

A mixture comprising 6-bromopyrazolo[1,5-a]pyridine-3-carboxylic acid (commercially available) (196 mg, 0.813 mmol) and thionyl chloride (2 ml, 27.4 mmol) was heated at 60° C. for 1 hr and concentrated in vacuo. To this was added 3-amino-4-methyl-N-(2-(4-methylpiperazin-1-yl)benzyl)benzamide (step 1) (220 mg, 0.651 mmol) and pyridine (5 ml). The reaction was stirred under nitrogen at room temperature for 2 hrs. The mixture was diluted with 10% MeOH in EtOAc and washed with water, sat NaHCO3, brine and concentrated in vacuo. The crude product was purified by chromatography on silica eluting with 0-20% 2M NH3 in MeOH/DCM to afford the title compound;

1. concentrationconcentrated in vacuo
2. washwashed with water
3. concentrationconcentrated in vacuo
4. customThe crude product was purified by chromatography on silica eluting with 0-20% 2M NH3 in MeOH/DCM