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Therapeutic Potential of 5-HT6 Receptor Agonists.
Surprisingly, some studies have shown that both 5-HT6R agonists and antagonists exert similar procognitive activities, and this article summarizes the hypotheses that could explain this paradox.
Modulating 5-HT4 and 5-HT6 receptors in Alzheimer's disease treatment.
This review will describe recent advances in the understanding of this modulation as well as the medicinal chemistry of 5- HT6R or 5-HT4R ligands from synthesis to ongoing clinical trials.
Copper-catalyzed iminoiodane-mediated aminolactonization of olefins: application to the synthesis of 5,5-disubstituted butyrolactones.
A copper(I)-catalyzed reaction of a variety of 4-aryl-pent-4-enoates with nosyliminoiodane generated in situ provides the corresponding 5-aryl-5-nosylamidomethylbutyrolactones. The reaction
Synthetic approaches to racemic porantheridine and 8-epihalosaline via a nitroso Diels-Alder cycloaddition/ring-rearrangement metathesis sequence.
The formation of the 2,6-trans-disubstituted piperidine backbone of porantheridine has been accomplished by addition of a Grignard reagent onto an N-benzylpiperidone followed by a highly diastereoselective reduction of the imminium intermediate in one pot.
Stereodivergent synthesis of piperidine alkaloids by ring-rearrangement metathesis/reductive lactam alkylation of nitroso Diels-Alder cycloadducts.
A general methodology for the stereoselective synthesis of 2-(2-hydroxyalkyl)piperidine alkaloids by ring-rearrangement metathesis of nitroso Diels-Alder cycloadducts is reported. The approach is
Copper-Catalyzed Iminoiodane-Mediated Aminolactonization of Olefins: Application to the Synthesis of 5,5-Disubstituted Butyrolactones.
Five- and six-membered heterocycles such as tetrahydrofurans, tetrahydropyrans, cyclic carbamates are obtained with good yields from the starting styrene-derived 1-propanoates or butanoates.