tert-butyl (3R)-3-aminopiperidine-1-carboxylate → (3R)-tert-butyl 3-((4-(5-(2,6-difluorophenyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-3-yl)-6-((4-methoxybenzyl)oxy)pyrimidin-2-yl)amino)piperidine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

A glass microwave reaction vessel was charged with 5-(2,6-difluorophenyl)-3-(6-(4-methoxybenzyloxy)-2-(methylsulfonyl)pyrimidin-4-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole (200 mg, 0.330 mmol) and (R)-tert-butyl 3-aminopiperidine-1-carboxylate (198 mg, 0.989 mmol) in NMP (2.0 mL). The reaction was stirred and heated in a Initiator microwave reactor (Personal Chemistry, Biotage AB, Inc., Upssala, Sweden) at 125° C. for 2 h. The mixture was diluted with water and the resulting suspension was filtered. The solid was washed with water and dried to give 115 mg of the crude product, which was used in the next step without further purification. MS (ESI, pos. ion) m/z: 727.1 (M+1).

Provenance & Evidence