Cesium carbonate → HCID 178480793, compound

Participants

Reaction Conditions

Reaction Steps

A microwave tube fitted with a stir bar was charged with tert-butyl((trans)-3-((2-chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)carbamate (260 mg, 0.55 mmol), 1,4-dioxane (3 mL), Cs2CO3 (452 mg, 1.4 mmol), Pd2(dba)3 (16 mg, 0.03 mmol), Xantphos (34 mg, 0.056 mmol) and 1-methyl-1H-pyrazol-4-amine (60 mg, 0.58 mmol). The tube was flushed with nitrogen gas and heated at 140° C. in a Biotage microwave reactor for 40 min. The product was purified via flash chromatography eluting with a gradient of 30%-100% EtOAc in heptanes to afford the title compound (115 mg, 39% yield) as an orange foam.

Provenance & Evidence