1-Hydroxybenzotriazole → 1-(3-(3,4-Dimethoxyphenethyl)-2-oxo-3,10-diazabicyclo[4.3.1]-decan-10-yl)-2-(3,4,5-trimethoxyphenyl)ethane-1,2-dione

Participants

Reaction Steps

To a solution of 3-(3,4-dimethoxyphenethyl)-3,10-diazabicyclo[4.3.1]decan-2-one (27 mg, 0.09 mmol) in 3 ml DCM was added sequentially 2-oxo-2-(3,4,5-trimethoxyphenyl) acetic acid (23 mg, 0.1 mmol), EDC-HCl (20 mg, 0.1 mmol), HOBt (14 mg, 0.1 mmol), TEA (10 mg, 0.1 mmol) at room temperature and stirred overnight. The reaction was quenched with saturated NH4Cl solution (5 ml), extracted with DCM (4×10 ml). The organic layers were dried over MgSO4 and concentrated in vacuo. The reaction mixture was purified with flash chromatography in EtOAc. TLC [EtOAc]: Rf=0.42

Provenance & Evidence