Current Medicinal Chemistry 2009-01-01

Recent developments in the chemistry of thebaine and its transformation products as pharmacological targets.

Sándor Berényi, Csaba Csutorás, Attila Sipos

Index: Curr. Med. Chem. 16(25) , 3215-42, (2009)

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Abstract

The most practical synthetic routes to the preparation of as important pharmaceuticals as oxycodone, naloxone, naltrexone, nalbuphine and buprenorphine have utilized the alkaloid, thebaine, as a starting material. This review intends to focus on chemical transformations of morphinans which resulted in morphinandiene derivatives with well-established and novel pharmacological potencies. These chemical transformations were mainly associated with the formation and substitution of the unique diene structure of the ring C of the morphinan backbone.