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

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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; dopamine activity; morphinandiene; opioid activity; orvinols

Document Type: Research Article


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

Publication date: September 1, 2009

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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