Tetrahydrofuran → HCID 86711158, compound

Participants

Reaction Steps

A solution of paliperidone (746.26 mg, 1.75 mmol) in THF (15 mL) was treated with 3-(Boc-amino)propyl bromide (500 mg, 2.10 mmol), 18-Crown-6 (231.25 mg, 0.874 mmol) and sodium hydride (60 w/w %, 139.97 mg, 3.5 mmol). The mixture was stirred at room temperature for 6 h. The solvent was removed under vacuum, dissolved in dichloromethane/water (50 mL/50 mL) and the aqueous layer extracted with dichloromethane (three times 50 mL). The combined organic layers were dried over Na2SO4, filtered and concentrated to give the title compound, which was used without further purification in the next step.

Provenance & Evidence