2-((R)-1-Amino-2-methyl-propyl)-3-benzyl-5,6-dimethyl-3-H-pyrimidin-4-one (0.500 g, 1.75 mMol) and 2H-isoindole-2-acetaldehyde [2913-97-5] (0.661 g 3.50 mMol) were dissolved in dichloroethane (20 mL). Glacial acetic acid was added (0.400 mL, 0.70 mMol) followed by sodium triacetoxy borohydride (0.942 g, 4.40 mMol). The reaction stirred at room temperature under nitrogen for 3.5 h. The reaction was quenched with NaHCO3 (sat. Aq.) and extracted with EtOAc (3×). The organic layer was evaporated under reduced pressure and purified by flash chromatography. (EtOAc/hexane 50–95% gradient) to give the title compound 420 mg (0.92 mMol) MS (ES) m/e 459 (M+H)+.
