N-[5-amino-2-[2-(dimethylamino)ethyl-methylamino]phenyl]acetamide → Acetamide, N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]phenyl]-

Participants

Reaction Conditions

Reaction Steps

In a 40mL vial (t=g) was 5-chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (200 mg, 0.86 mmol), N-(5-amino-2-((2-(dimethylamino)ethyl)(methyl)amino)phenyl)acetamide (214 mg, 0.86 mmol), and cesium carbonate (363 mg, 1.11 mmol) in DMA (0.5 mL) ([VOLUME]),Pd2(dba)3 (39.2 mg, 0.04 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (49.5 mg, 0.09 mmol) were added. to give a brown suspension. The vial was filled with N2, 150C microwave for 30 min. LCMS showed completion. concentrated. loaded on ISCO (Hex to Hex:EtOAc To EtOAc:MeOH=10:1 to EtOAc:MeOH:Et3N=10:1:0.1) to give yellow sticky oil. tried to use EtOAc(1 mL) as solvent to make the product to form crys. finally the solid was formed and washed with EtOA (1mL) and Et2O(2mL) to give 86mg white solid NMR LCMS are OK

Provenance & Evidence