A convergent strategy towards febrifugine and related compounds.

We report a modular five step synthetic route to the febrifugines that employs 2-(chloromethyl)allyl-trimethylsilane as a conjunctive reagent for the coupling of the piperidine and quinazolinone groups. We also demonstrate the application of a recent Rh-catalyzed quinazolinone synthesis for the facile generation of febrifugine analogs.

Synthesis of aminopyrazoles from sydnones and ynamides.

Aminopyrazoles are prepared from readily accessible sydnones and sulfonyl ynamides using either a copper-mediated sydnone alkyne cycloaddition (CuSAC) or in situ generated strained cyclic ynamides.

Recent developments in transition metal catalysis for quinazolinone synthesis.

Quinazolinones are an important class of heteroaromatic compound, and they are prevalent in a variety of important bio-active scaffolds. Traditionally, their synthesis has been achieved via classical condensation procedures, however over recent years catalytic methodologies have emerged as effective alternatives. This review examines recent developments in the employment of catalytic approaches towards this highly important heterocyclic motif.