Succinimido 1-t-butoxycarbonylpiperidine-4-carboxylate → tert-butyl 4-({[1-methyl-5-(tritylamino)-1H-pyrazol-4-yl]amino)carbonyl)-1-piperidinecarboxylate

Participants

Reaction Steps

To a solution of 1-methyl-N5-trityl-1H-pyrazole-4,5-diamine (4 g) in dichloromethane (100 ml) was added tert-butyl 4-{[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl}-1-piperidinecarboxylate (4.05 g), and the mixture was refluxed for 72 hours. The reaction mixture was washed successively with water 10% aqueous citric acid solution, water and brine. The extract was dried over anhydrous magnesium sulfate, filtered and concentrated in vacuo to give tert-butyl 4-({[1-methyl-5-(tritylamino)-1H-pyrazol-4-yl]amino}carbonyl)-1-piperidinecarboxylate (1.806 g).

Provenance & Evidence