Koolpe, Gary A.; Nelson, Wendel L.; Gioannini, T. L.; Angel, Lloyd; Simon, Eric J. published an article in 1984, the title of the article was Diastereomeric 6-desoxy-6-spiro-α-methylene-γ-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted Michael acceptor ligand.Quality Control of trimethyloxosulphonium chloride And the article contains the following content:
The title compounds I and II (R = Me or cyclopropylmethyl) were prepared by sequence reaction starting with direct alkylation of the diacetate ester of the parent ketone by the Reformatskii reagent prepared from Me α-(bromomethyl)acrylate [4224-69-5], and their affinity for opioid binding sites was determined in crude rat brain membrane preparation by competition against [3H]naltrexone in presence and absence of Na+. 6α-(2-Carboxyallyl)-17-(cyclopropylmethyl)-4,5α-epoxy-3,6β,14-trihydroxymorphinan-γ-lactone (II; R = cyclopropylmethyl) [92398-30-6] was the most potent compound showing a 50% inhibition of binding at 5 nM. The data suggest a receptor nucleophile such as SH is located where it can add to the α,β-unsaturated carbonyl system of the above compound The experimental process involved the reaction of trimethyloxosulphonium chloride(cas: 5034-06-0).Quality Control of trimethyloxosulphonium chloride
The Article related to naltrexone butyrolactone diastereomer preparation, oxymorphone butyrolactone diastereomer preparation, opioid receptor binding morphinanone derivative, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Quality Control of trimethyloxosulphonium chloride
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