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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Recent Developments in the Chemistry of Thebaine and its Transformation Products as Pharmacological Targets

Author(s): Sandor Berenyi, Csaba Csutoras and Attila Sipos

Volume 16 , Issue 25 , 2009

Page: [3215 - 3242] Pages: 28

DOI: 10.2174/092986709788803295

Price: $65


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.

Keywords: Thebaine, morphinandiene, opioid activity, dopamine activity, orvinols

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