Cesium carbonate → HCID 89923930, compound

Participants

Reaction Conditions

Reaction Steps

A oven-dried 10 ml microwave flask was loaded with 2-amino-4-(ethyl(4-methoxybenzyl)amino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (16 mg, 0.049 mmol), (3R,4R)-methyl 4-((3-bromo-2-chloro-5-cyanophenyl)amino)-3-hydroxypiperidine-1-carboxylate (19 mg, 0.049 mmol), Pd(OAc)2 (3 mg, 0.013 mmol), XANTPHOS (8 mg, 0.014 mmol) and Cs2CO3 (50 mg, 0.153 mmol). The flask was evacuated and back-filled with nitrogen 4 times. 1,4-Dioxane (0.5 mL) was added and the flask was again evacuated and back-filled with nitrogen 4 times, then heated with stirring to 70° C. for 2 hours. The reaction is complete by LCMS analysis. The reaction mixture was diluted with EtOAc, washed with water, brine and dried over Na2SO4. The solvent removed to afford (3R,4R)-methyl 4-((2-chloro-5-cyano-3-((7-cyano-4-(ethyl(4-methoxybenzyl)amino)imidazo[2,1-f][1,2,4]triazin-2-yl)amino)phenyl)amino)-3-hydroxypiperidine-1-carboxylate (30.9 mg). The material was used as is.

Provenance & Evidence