Expeditious synthesis of ‘P’-protected macrocycles en route to lanthanide chelate metal complexes

Phosphonic acid appended tetraazacyclododecane (cyclen)-based macrocycles are attractive metal-ion chelators for diagnostic imaging and therapeutic delivery. Here, we report a novel P-protected methodology that facilitates the rapid synthesis and purification of targeted phosphonic acid bearing macrocycles. Purification of these intermediates is facile, and deprotection using neat TFA is rapid, yet mild enough to preserve the integrity of delicate peptides and/or targeting moieties.     

Rapid, microwave-assisted organic synthesis of selective BRAF inhibitors for preclinical cancer research

We report dramatically improved total syntheses of two highly selective ^V600EBRAF inhibitors, PLX4720 and PLX4032, that leverages microwave-assisted organic synthesis (MAOS). Compared with previously reported approaches, our novel MAOS method significantly reduces overall reaction time without compromising yield. In addition to providing a gram-scale route to these compounds for preclinical oncology research, we anticipate this approach could accelerate the synthesis of azaindoles in high-throughput, library-based formats.     

Zur Erzielung hoher Vakua im Exsikkator

Ohne Zusammenfassung     

Irrationality of linear combinations of eigenvectors

A givenn ×n matrix of rational numbers acts onC ^π and onQ ^π. We assume that its characteristic polynomial is irreducible and compare a basis of eigenvectors forC ^π with the standard basis forQ ^π. Subject to a hypothesis on the Galois group we prove that vectors from these two bases are as independent of each other as possible.     

Efficient generation of high-power VUV ultrashort pulses by four-wave mixing

We report the generation of ultra-short pulses in the VUV (λ = 173.5 nm) using a four-wave mixing technique in magnesium vapour. Using a mode-locked ruby laser as the original source, conversion efficiencies of up to 0.2% and powers of 0.3 MW were obtained.