Dicyclohexylcarbodiimide → HCID 86711156, compound

Participants

Reaction Steps

A solution of Paliperidone (1.0 g, 2.34 mmol) in dichloromethane (20 mL) was treated with Boc-b-Ala-OH (443.65 mg, 2.34 mmol), dicyclohexylcarbodiimide (483.79 mg, 2.34 mmol) and N,N-dimethyl-4-pyridinamine (14.32 mg, 0.117 mmol). The reaction was stirred at room temperature under argon atmosphere. After 18 h, the reaction mixture was poured into an aqueous saturated sodium bicarbonate solution (20 mL) and the aqueous layer extracted with dichloromethane (three times 20 mL). The combined organic layers were dried over MgSO4, filtered and concentrated. The residue was purified by silica gel chromatography (elution with dichloromethane/methanol (95/5) to give the title compound. ESI-MS (M+1) 598.

Provenance & Evidence