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

[ Vol. 16 , Issue. 25 ]

Author(s):

Sandor Berenyi, Csaba Csutoras and Attila Sipos   Pages 3215 - 3242 ( 28 )

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.

Keywords:

Thebaine,morphinandiene,opioid activity,dopamine activity,orvinols

Affiliation:

, , Department of Organic Chemistry, University of Debrecen, P. O. Box 20, H-4010, Debrecen, Hungary.



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