Formic Acid → methyl 2-amino-6,7-dihydro-5H-cyclopenta[d]pyrimidine-5-carboxylate

Participants

Reaction Conditions

Reaction Steps

Triethylamine (3.20 mL, 23.0 mmol) was added to a solution of methyl 2-amino-4-chloro-6,7-dihydro-5H-cyclopenta[d]pyrimidine-5-carboxylate (2.11 g, 9.27 mmol) in dioxane (42 mL) followed by formic acid (0.89 mL, 22.28 mmol) and [1,1′-bis(diphenylphosphino)ferrocene]-dichloropalladium(II) (660 mg, 0.902 mmol). The reaction mixture was heated at 100° C. in a sealed tube overnight. The solvent was evaporated. The residue was purified by chromatography on silica (220 g+125 g cartridges) using CH2Cl2: MeOH 95:5 to afford the title compound which was used without further purification in the next step.

Provenance & Evidence