Potassium Carbonate → 3-(5-Bromo-pyrimidin-2-ylamino)-piperidine-1-carboxylic acid tert-butyl ester

Participants

Reaction Steps

To a solution of (+/−)-3-amino-1-N-Boc-piperidine (1 g) in dry o-xylene (20 mL) were added successively 5-bromo-2-chloropyrimidine (965 mg), anhydrous K2CO3 (1.38 g), DIEA (3.42 mL). The reaction mixture was stirred at reflux for 3 d under nitrogen. After cooling to RT, the brown suspension was filtered and the filtrate was concentrated to yield a crude brown-orange oil. FC (EA/n-heptane: 3/7) gave 850 mg (46%) of the title compound as a light brown solid.

Provenance & Evidence