Hydrogen-bond inter­actions in morpholinium bromide

In the title compound, C4H10NO+·Br−, which was synthesized by dehydration of diethano­lamine with HBr, morpholinium and bromide ions are linked into chains by N—H⋯Br hydrogen bonds describing a C 2 1(4) graph-set motif. Weaker bifurcated N—H⋯Br inter­actions join centrosymmetrically related chains through alternating binary graph-set R 4 2(8) and R 2 2(4) motifs, to form ladders along [100]. In addition, C—H⋯O inter­actions between centrosymmetric morpholinium cations link ladders, via (8) motifs, to yield sheets parallel to (101), which in turn are crosslinked by weak C—H⋯O inter­actions, related across a glide plane, to form a three-dimensional network

Palladium–mediated organofluorine chemistry

Producción CientíficaThe substitution of fluorine for hydrogen in a molecule may result in profound changes in its properties and behaviour. Fluorine does not introduce special steric constraints since the F atom has a small size. However, the changes in bond polarity and the possibility of forming hydrogen bonds with other hydrogen donor fragments in the same or other molecules, may change the solubility and physical properties of the fluorinated compound when compared to the non-fluorinated one. Fluorine forms strong bonds to other elements and this ensures a good chemical stability. Altogether, fluorinated compounds are very attractive in materials chemistry and in medicinal chemistry, where many biologically active molecules and pharmaceuticals do contain fluorine in their structure and this has been shown to be essential for their activityJunta de Castilla y León (programa de apoyo a proyectos de investigación – Ref. VA302U13)Junta de Castilla y León (programa de apoyo a proyectos de investigación – Ref. VA256U13

The synthesis of new fluorinated or nonfluorinated sugar phosphonates and phosphoramidates as building blocks in the synthesis of modified hyaluronic acid subunits

<p></p> <p>The synthesis of several new fluorinated or nonfluorinated sugar phosphonates and phosphoramidates as building blocks for the synthesis of modified hyaluronic acid subunits is described. These compounds were prepared from d-glucose and d-glucosamine hydrochloride. The syntheses of phosphonates and phosphoramidates are based on arbuzov and staudinger reactions. The products were fully characterized by ¹H, ¹³C, ¹⁹F, ³¹P NMR, and ESI MS spectroscopy.</p

Luck and hard work in drug discovery

Luck is one of the critical factors determining outcome of many activities we are involved in. In chemistry, and specifically in drug discovery a strike of luck can determine a successful study outcome leading to an approval of potentially blockbuster drug consequently offering a new treatment option for patients in need. On the other hand, lack of luck can often result in termination of activities, wasted resources and years of studies and often have negative impact on a fate of companies and its employees. In a similar fashion, hard work is critical for one’s success. It is not meant in a literal fashion, but rather from the perspective of “going the extra mile” in scientific research and development. It is meant as a proper approach to analysis of study outcome and understanding the reasons “why”, rather than accepting simply yes/no outcomes. Below article discusses two instances where certain level of luck and extra effort invested in understanding of widely available results led to development of two novel therapeutics in oncology field. Described stories deal with development of Abraxane, novel formulation of paclitaxel commercialized by Abraxis Bioscience as well as enzalutamid (Xtandi®) discovered at UCLA and developed and commercialized by Medivation and Astellas Pharma