Toll-Like Receptor 4 (TLR4) is an innate immune system receptor implicated in opioid tolerance and addiction. Unnatural enantiomers of morphinans such as (+)-naloxone have been found to be a TLR4 antagonist in cell studies. A concise and versatile synthesis of unnatural enantiomers of morphinan derivatives based on the route developed by Kenner Rice at the National Institutes of Health will be presented along with potency data of the derivatives.

Synthesis of unnatural enantiomers of morphinan derivatives as toll-like receptor 4 inhibitors

249th National Meeting (2015)

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