Cesium carbonate → tert-butyl 4-(N-(3-(5-fluoro-1-methylindolin-6-yl)-1-isopropyl-1H-pyrrolo[2,3-b]pyridin-4-yl)sulfamoyl)piperidine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

A microwave vial was charged with tert-butyl 4-sulfamoylpiperidine-1-carboxylate (331 mg, 1.252 mmol), 4-bromo-3-(5-fluoro-1-methylindolin-6-yl)-1-isopropyl-1H-pyrrolo[2,3-b]pyridine (D37) (324 mg, 0.834 mmol), Pd2(dba)3 (76 mg, 0.083 mmol), xantphos (97 mg, 0.167 mmol) and cesium carbonate (816 mg, 2.503 mmol). This was suspended in 1,4-dioxane (7 mL) and degassed under nitrogen atmosphere for 10 mins before subjected to microwave heating at 130° C. for 30 mins. The reaction mixture was filtered through celite (washing with ethyl acetate). The filtrate was removed in vacuo to give a residue which was purified using chromatography on silica (eluted with 0-20% ethyl acetate/DCM) to afford the title compound (450 mg). LCMS (A): m/z (M+H)+ 572, C29H38FN5O4S requires 571 (acidic).

Provenance & Evidence