Trifluoroacetic acid → 8-Azetidin-3-ylmethyl-2-(2-ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purine

Participants

Reaction Steps

To a solution of tert-butyl 3-((9-methyl-2-(2-ethyl-1H-benzo[d]imidazol-1-yl)-6-morpholino-9H-purin-8-yl)methyl)azetidine-1-carboxylate (0.64 g, 1.2 mmol) in DCM (10 mL) was added trifluoroacetic acid (1.0 mL, 13 mmol) The reaction mixture was then stirred at room temperature for 1 hour. The reaction mixture was then evaporated to dryness. The residue was then re-dissolved in MeOH and neutralized by adding a 2M NH3 in MeOH. The solution was then concentrated and purified by flash chromatography using a KP—NH2 column (0-10% MeOH in DCM) to give 530. LCMS m/z: 433.2 (MH+)

Provenance & Evidence