An oxidative cascade cyclization of β-keto esters has been developed for the construction of the tricyclic picrotoxane motif in a single step, and DFT calculations suggested a possible cationic cyclization mechanism. This cascade cyclization can be operated on a 20 g scale to obtain a 77% total yield of the tricyclic products, which in turn can be converted to versatile intermediates for further elaboration to picrotoxanes and their structurally related compounds.

Aculeatin A, isolated from the plant Amomum aculeatum, is a dispirocyclic compound having antimalarial activity. We describe a novel synthetic approach to aculeatin A via a stepwise strategy.

Abstract. (R)-tert-butyl 4-formyl-2,2-dimethylthiazolidine-3-carboxylate is an imntermediate of S-jaspine B known as a potential substitution of pachastrissamine (jaspine B) which shows effective biological activity. Herein we describe an elegant straightforward synthetic path for this attractive molecule intermediate.