Over recent decades, global warming has led to sustained glacier mass reduction and the formation of glacier lakes dammed by potentially unstable moraines. When such dams break, devastating Glacial Lake Outburst Floods (GLOFs) can occur in high mountain environments with catastrophic effects on populations and infrastructure. To understand the occurrence of GLOFs in space and time, build frequency-magnitude relationships for disaster risk reduction or identify regional links between GLOF frequency and climate warming, comprehensive databases are critically needed.
View Article and Find Full Text PDF2-Arylethylamines are presented in several natural bioactive compounds, as well as in nitrogen-containing drugs. Their ability to surpass the blood-brain barrier makes this family of compounds of especial interest in medicinal chemistry. Asymmetric methodologies towards the synthesis of 2-arylethylamine motives are of great interest due to the challenges they may present.
View Article and Find Full Text PDFThe concept of bioisostere replacement is of paramount importance in medicinal chemistry, as it can be employed as a rational to expand bioactive chemical space to tackle lead optimization issues like lack of potency, efficacy, and selectivity or pharmacokinetic/dynamic issues. One of the most important building blocks (in the sense of participating in a vast area of chemical space of biological importance) in medicinal chemistry is the 2-phenethyl moiety, a key component of diverse drug-like entities. Although the core 2-phenethylamine structure has been recognized by the drug discovery community, little attention has been given to the various ring-based rescaffolding procedures that can be conducted with this unit.
View Article and Find Full Text PDFThe development of methods to allow the selective acylative dynamic kinetic resolution (DKR) of tetra-substituted lactols is a recognised synthetic challenge. In this manuscript, a highly enantioselective isothiourea-catalysed acylative DKR of tetra-substituted morpholinone and benzoxazinone-derived lactols is reported. The scope and limitations of this methodology have been developed, with high enantioselectivity and good to excellent yields (up to 89 %, 99 : 1 er) observed across a broad range of substrate derivatives incorporating substitution at N(4) and C(2), di- and spirocyclic substitution at C(5) and C(6), as well as benzannulation (>35 examples in total).
View Article and Find Full Text PDFThe primary goal of paleoflood hydrology is to estimate the frequency and magnitude of past floods. Botanical evidence, and particularly scars on trees, has been used repeatedly as paleostage indicators to reconstruct peak discharges and flood height. Yet, these reconstructions depend on the presence of visible scars on tree stems which tend to be masked as trees grow older.
View Article and Find Full Text PDFA concise review covering updated presence and role of 2-phenethylamines in medicinal chemistry is presented. Open-chain, flexible alicyclic amine derivatives of this motif are enumerated in key therapeutic targets, listing medicinal chemistry hits and appealing screening compounds. Latest reports in discovering new bioactive 2-phenethylamines by research groups are covered too.
View Article and Find Full Text PDFEzetimibe is a well-known drug that lowers blood cholesterol levels by reducing its absorption in the small intestine when joining to Niemann-Pick C1-like protein (NPC1L1). A ligand-based study on ezetimibe analogues is reported, together with one-hit synthesis, highlighted in the study. A convenient asymmetric synthesis of (2,3)--α-()-methylbenzyl-3-methoxycarbonylethyl-4-methoxyphenyl β-lactam is described starting from Baylis-Hillman adducts.
View Article and Find Full Text PDFAlmost all chemical elements have been made by nucleosynthetic reactions in various kind of stars and have been accumulated along our cosmic history. Among those elements, the origin of phosphorus is of extreme interest because it is known to be essential for life such as we know on Earth. However, current models of (Galactic) chemical evolution under-predict the phosphorus we observe in our Solar System.
View Article and Find Full Text PDFThe asymmetric synthesis of a compound with the cyclopentan[c]pyran core of iridoid natural products in four steps and 40% overall yield is reported. Our methodology includes a one-pot tandem domino reaction which provides a trisubstituted cyclopentane with five new completely determined stereocenters, which were determined through 2D homo and heteronuclear NMR and n.O.
View Article and Find Full Text PDFActa Crystallogr E Crystallogr Commun
April 2017
The title compound, CHNO, was prepared by CAN [cerium(IV) ammonium nitrate] oxidation of the corresponding β-lactam. The dihedral angle between the benzene rings is 13.3 (4)° and the C-N-C(=O)-C torsion angle is 176.
View Article and Find Full Text PDFA series of 33 different polycyclic aromatic hydrocarbons (PAHs) were studied by far infrared spectroscopy (terahertz spectroscopy) in the spectral range comprised between 600 and 50 cm(-1). In addition to common PAHs like naphthalene, anthracene, phenanthrene, fluoranthene, picene, pyrene, benzo[α]pyrene, and perylene, also quite unusual PAHs were studied like tetracene, pentacene, acenaphtene, acenaphtylene, triphenylene, and decacyclene. A series of alkylated naphthalenes and anthracenes were studied as well as methypyrene.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
December 2010
Oleum (fuming sulphuric acid), a well known superacid, was used as medium for the generation of the radical cation of a series of selected PAHs. The resulting radical cation spectra were studied by electronic absorption spectroscopy. Not only common PAHs like naphthalene, anthracene, tetracene, pentacene, perylene, pyrene, benzo[a]pyrene, phenanthrene and picene were studied but also the less common and very large PAHs relevant also for the astrochemical research, like coronene, hexabenzocoronene, quaterrylene, dicoronylene and a coronene oligomer.
View Article and Find Full Text PDFA long-debated issue concerning the nucleosynthesis of neutron-rich elements in asymptotic giant branch (AGB) stars is the identification of the neutron source. We report intermediate-mass (4 to 8 solar masses) AGB stars in our Galaxy that are rubidium-rich as a result of overproduction of the long-lived radioactive isotope (87)Rb, as predicted theoretically 40 years ago. This finding represents direct observational evidence that the (22)Ne(alpha,n)(25)Mg reaction must be the dominant neutron source in these stars.
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