AI Article Synopsis
- * Researchers have created a new method for this -demethylation step that doesn't need any harsh reagents or catalysts, using anodic oxidation instead.
- * This new procedure allows for easy conversion of intermediates into target nor-opioids with high yields, making the process safer and more efficient.
Article Abstract
The most challenging step in the preparation of many opioid antagonists is the selective -demethylation of a 14-hydroxymorphinan precursor. This process is carried out on a large scale using stoichiometric amounts of hazardous chemicals like cyanogen bromide or chloroformates. We have developed a mild reagent- and catalyst-free procedure for the -demethylation step based on the anodic oxidation of the tertiary amine. The ensuing intermediates can be readily hydrolyzed to the target nor-opioids in very good yields.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7498191 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.0c02424 | DOI Listing |
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