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Total Synthesis of Northebaine, Normorphine, Noroxymorphone Enantiomers and Derivatives via N-Nor Intermediates

Posted Jul 31 2008 5:00pm

Description of Invention:
A new synthetic process has been found in which nordihydrocodeinone, an early intermediate in the total synthesis of codeine and related compounds, is easily formed into a number of N-nor compounds. These N-nor compounds can be used as precursors in the formation of narcotics, narcotic antagonists, or narcotic agonist-antagonists.

The manufacture of drugs of this type, such as northebaine or normorphine, can now be done without the use of thebaine as starting material. The syntheses have fewer steps than previous methods, and also have high yields. In addition, very significant simplification of existing thebaine based processes for the manufacture of opiates can be expected.

Applications:
Potential new methodology for the synthesis of intermediates for drugs including naloxone, naltrexone, percodan and nalbuphine.

Inventors:
Kenner C Rice (NIDDK)


Licensing Status:
Available for licensing.


Portfolios:
Central Nervous System
Central Nervous System - Therapeutics
Central Nervous System - Research Materials



For Additional Information Please Contact:
Charlene Sydnor Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: sydnorc@mail.nih.gov
Phone: 301-435-4689
Fax: 301-402-0220


Ref No: 1806

Updated: 08/2008

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