N-benzyl-N-methyl-3-azabicyclo[3.2.1]octan-8-amine → tert-butyl (1S)-2-{8-[benzyl(methyl)amino]-3-azabicyclo-[3.2.1]oct-3-yl}-1-[(4-cyanophenoxy)methyl]ethylcarbamate

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl (2S)-2-[(4-cyanophenoxy)methyl]-1-aziridinecarboxylate (see step (iii) above; 1.26 g, 4.6 mmol) and N-benzyl-N-methyl-3-azabicyclo[3.2.1]octan-8-amine (see step (vii) above; 1.05 g, 4.6 mmol) in IPA (15 mL) was stirred at 60° C. overnight. The solvent was evaporated and the residue purified by chromatography on silica gel, eluting with DCM:MeOH (20:1). This gave 1.8 g (78%) of the subtitle compound

Provenance & Evidence