Cesium carbonate → HCID 86712733, compound

Participants

Reaction Conditions

Reaction Steps

A suspension of 2-(2-(2-(2-chloro-5-methylpyrimidin-4-yl)ethyl)phenyl)acetamide (K6) (0.200 g, 0.690 mmol), tert-butyl (1-(4-aminophenyl)ethyl)carbamate (A131) (0.326 g, 1.38 mmol), Pd(OAc)2 (3 mg, 0.01 mmol), Cs2CO3 (0.675 g, 2.07 mmol) and Xantphos (16 mg, 0.028 mmol) in 1,4-dioxane (3 mL) was heated under microwave irradiation at 105° C. for 6 hours. The resulting mixture was filtered through a plug of silica gel, washing with 20% MeOH in K1 DCM and then the volatiles evaporated in vacuo. The residue was purified using silica gel column chromatography (CombiFlash Rf, 12 g SiO2 Cartridge, 5-80% EtOAc in cyclohexane) to give the title compound A132 as a white solid (0.099 g, 29%); LCMS-B: rt 6.832 min; m/z 490 [M+H]+.

Provenance & Evidence