Carbonic acid, bis(1,1-dimethylethyl) ester → Tert-butyl 4-((6-aminopyridin-2-yl)methyl)piperazine-1-carboxylate

Participants

Reaction Steps

To a solution of 6-(piperazin-1-ylmethyl)pyridin-2-amine 85 in THF was added di-tert-butyl carbonate (1 eq) and 4-(dimethyl)aminopyridine (catalytic). The reaction mixture was stirred at room temperature for 18 h. It was then concentrated under reduced pressure. Pentane was added and the resulting solid was collected by filtration and dried to afford 86. The Boc protecting group could be removed after coupling with the appropriate carboxylic acid by treatment with TFA/CH2Cl2 for 12 h.

Provenance & Evidence