Disclosed is a process for the preparation of the compound of formula (I):
which comprises reacting a compound of formula (II):
with acylating agent of formula (IV) in the presence of orthoester of formula (III) in an aprotic solvent:
The process may be used for synthesizing derivatives of fentanyl. Specifically set out are pathways for synthesizing remifentanil and carfentanil. The disclosed process require fewer steps and produce a greater yield of products than methods reported in the prior art.
本发明涉及一种制备式(I)化合物的方法,其中包括在无极性溶剂中,在式(III)的正酯化试剂的存在下,将式(II)的化合物与正酯化试剂的式(IV)反应。该方法可用于合成
芬太尼的衍
生物。具体地,本发明揭示了合成
瑞芬太尼和
芬太尼的途径。所揭示的方法比先前报道的方法需要更少的步骤,并且产量更高。