Given the prevalence of nitrogen-containing heterocycles in commercial drugs, selectively incorporating a single nitrogen atom is a promising scaffold hopping approach to enhance chemical diversity in drug discovery libraries. We harness the distinct reactivity of sulfenylnitrenes, which insert a single nitrogen atom to transform readily available pyrroles, indoles, and imidazoles into synthetically challenging pyrimidines, quinazolines, and triazines, respectively. Our additive-free method for skeletal editing employs easily accessible, benchtop-stable sulfenylnitrene precursors over a broad temperature range (-30 to 150°C).
View Article and Find Full Text PDFClimate modeling suggests that achieving international climate goals requires a reduction in current CO emissions by over 90%, with any remaining emissions to be addressed through carbon dioxide removal (CDR) solutions. Sixteen CDR strategies are evaluated by integrating technical potential, environmental, social, and governance (ESG) criteria, along with sequestration permanence. This evaluation, conducted by ENGIE's scientific council using an interdisciplinary Delphi panel methodology, proposes a "quality" measure for each technology.
View Article and Find Full Text PDFThioglycoside activation, crucial for oligosaccharide synthesis, faces challenges with the need for stoichiometric promoters, additives, and cryogenic conditions, particularly in stereoselective 1,2--linkage formation. This study introduces a carbene-based catalytic method using Cu(OTf) for thioglycoside activation, enabling efficient 1,2--furanosylation in ribose and arabinose. The method is orthogonal to conventional thioglycoside and alkyne donors, accommodates sterically demanding acceptors, and achieves stereoselectivity independent of the donor anomeric configuration and C2-protecting groups, with copper chelation playing a key role.
View Article and Find Full Text PDFObjectives: While clinical practice guidelines recommend that oncologists discuss goals of care with patients who have advanced cancer, it is estimated that less than 20% of individuals admitted to the hospital with high-risk cancers have end-of-life discussions with their providers. While there has been interest in developing models for mortality prediction to trigger such discussions, few studies have compared how such models compare with clinical judgment to determine a patient's mortality risk.
Methods: This study is a prospective analysis of 1,069 solid tumor medical oncology hospital admissions ( = 911 unique patients) from February 7 to June 7, 2022, at Memorial Sloan Kettering Cancer Center.