The efficient palladium-catalyzed synthesis of a range of substituted 2H-Indazoles via C-H arylation is reported. Reactions are performed on water and provide a direct and mild route toward 2,3-diaryl indazoles of widespread biological significance.

Selective activation of peripheral cannabinoid CB1 receptors has the potential to become a valuable therapy for chronic pain conditions as long as central nervous system effects are attenuated. A new class of cannabinoid ligands was rationally designed from known aminoalkylindole agonists and showed good binding and functional activities at human CB1 and CB2 receptors. This has led to the discovery of a novel CB1/CB2 dual agonist, naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone (13), which displays good oral bioavailability, potent antihyperalgesic activity in animal models, and limited brain penetration.

No abstract

The biomimetic synthesis of the manzamine-related alkaloid keramaphidin B is described. The key intramolecular Diels ± Alder reaction proposed in the Baldwin and Whitehead hypothesis is demonstrated. An investigation of the modified biomimetic hypothesis proposed by Marazano et al. is also reported. Finally, an alternative synthesis of keramaphidin B by Grubbs methathesis is presented.

Over the past decade there has been an upsurge in the discovery of biologically active natural products from marine sponges. [1] In comparison to terrestrial plant and microbial