Access to 1H-indazoles, 1H-benzoindazoles and 1H-azaindazoles from (het)aryl azides: a one-pot Staudinger-aza-Wittig reaction leading to N-N bond formation?

The synthesis of various substituted 1H-indazoles is reported through N-N bond formation from an iminophosphorane derivative. Supported by control experiments, an original Staudinger-aza-Wittig tandem mechanism is proposed for this transformation.

PET tracers for imaging brain α7 nicotinic receptors: an update.

Positron emission tomography (PET) molecular imaging of brain targets is a powerful tool to diagnose, follow up, and develop treatments and personalized medicine for a number of acute and chronic brain disorders. The availability of ß+ emitter tracers labelled with [(11)C] or [(18)F] having optimal characteristics of affinity and selectivity for alpha-7 nicotinic receptors (α7R) has received considerable attention, due to the major implication of these receptors in brain functions. The aim of this review is to identify the interest and need for the in vivo exploration of α7R by PET molecular imaging, which tools are currently available for this and how to progress.

An efficient synthetic approach to highly conjugated porphyrin-based assemblies containing a bipyridine moiety

[structure: see text] An efficient and potential stepwise strategy involving the mixed sequence of Stille and Wittig-Horner reactions was used for the preparation of a polyene-substituted bis-porphyrin incorporating a bipyridine moiety.

Chemical synthesis and cytotoxicity of some azinomycin analogues devoid of the 1-azabicyclo[3.1.0]hexane subunit.

A series of compounds related to the left-hand domain of the azinomycins have been made and evaluated for cytotoxic activity against a small panel of human tumour cell lines. The epoxide ring is shown to be essential for biological activity. Cytotoxicity is also shown to be sensitive to changes in the substitution pattern on the aromatic ring and the amide group.