An Efficient, Optimized Synthesis of Fentanyl and Related Analogs

作者:Valdez Carlos A; Leif Roald N; Mayer Brian P*
来源:PLos One, 2014, 9(9): e108250.
DOI:10.1371/journal.pone.0108250

摘要

The alternate and optimized syntheses of the parent opioid fentanyl and its analogs are described. The routes presented exhibit high-yielding transformations leading to these powerful analgesics after optimization studies were carried out for each synthetic step. The general three-step strategy produced a panel of four fentanyls in excellent yields (73-78%) along with their more commonly encountered hydrochloride and citric acid salts. The following strategy offers the opportunity for the gram-scale, efficient production of this interesting class of opioid alkaloids.

  • 出版日期2014-9-18