Diisopropylethylamine → [(R)-1-(6-fluoro-7-methyl-1-phenyl-1H-benzoimidazol-2-yl)-2-methoxyethyl]-[9-(tetrahydropyran-2-yl)-9H-purin-6-yl]amine

Participants

Reaction Conditions

Reaction Steps

A mixture of (R)-1-(6-fluoro-7-methyl-1-phenyl-1H-benzoimidazol-2-yl)-2-methoxyethylamine (270 mg, 0.9 mmol), 6-chloro-9-(tetrahydropyran-2-yl)-9H-purine (258 mg, 1.08 mmol) and DIPEA (308 μL, 1.8 mmol) in n-butanol (5 mL) was heated at 90° C. in a sealed vial for 18 h. After cooling to RT, the volatiles were removed under reduced pressure and the resulting residue purified by column chromatography (Si—PCC, gradient 0-10% MeOH in EtOAc) to afford [(R)-1-(6-fluoro-7-methyl-1-phenyl-1H-benzoimidazol-2-yl)-2-methoxyethyl]-[9-(tetrahydropyran-2-yl)-9H-purin-6-yl]amine: LCMS (Method C): RT 3.38 min [M+H]+ 502.2.

Provenance & Evidence