TEMPO-Mediated Dehydrogenative Hydroxyfluoroalkylation of Arylamines with Polyfluorinated Alcohols.

An efficient 2,2,6,6-tetramethylpiperidinooxy (TEMPO)-mediated hydroxyfluoroalkylation of arylamines with polyfluorinated alcohols via a radical-triggered C(sp2)-H/C(sp3)-H dehydrogenative cross-coupling process was developed. This transformation features simple operation, high atom economy, broad substrate compatibility, and excellent regioselectivity, leading to a series of hydroxyfluoroalkylated arylamine derivatives. Importantly, these synthetic products were further used to evaluate the antitumor activity in cancer cell lines by Cell Counting Kit-8 assay and the outcomes indicated that some compounds show a potent antiproliferative effect.

KBrO3-Promoted Cross-Dehydrogenative Coupling Reaction: An Odorless Regioselective Sulfenylation of Imidazoheterocycles in Water.

A regioselective metal-free sulfenylation of imidazoheterocycles with heterocyclic thiols or thiones has been achieved using a cross-dehydrogenative coupling method in water. In addition, the procedure has several advantages including green solvents, free of foul-smelling sulfur sources, and mild conditions, thus providing considerable application potential in the pharmaceutical industry.

Synthesis of Lactams via Ir-Catalyzed C-H Amidation Involving Ir-Nitrene Intermediates.

x-membered lactams were synthesized via either an amidation of sp3 C-H bonds or an electrophilic substitution of arenes via Ir-nitrene intermediates. With the employment of a readily available iridium catalyst in dichloromethane or hexafluoro-2-propanol, a wide range of lactams were synthesized in good to excellent yields with high selectivity.

Transition metal mediated carbonylative benzannulations.

In carbonylative benzannulations, feedstock carbon monoxide is converted to a benzene ring, which is one of the most fundamentally important and common rings in natural products and pharmaceutical compounds. Carbon monoxide, however, is rather inert in the absence of transition metals. Historically, carbonylative benzannulations have been mediated by stoichiometric chromium and iron in the form of Fischer carbenes. Recently, a number of transition metal-catalyzed carbonylative benzannulations have been developed, and almost all of them involve rhodium catalysts. This review will briefly discuss the mechanism and applications of carbonylative benzannulations involving Fischer carbenes and compare them with the more recent transition metal-catalyzed processes, including [3 + 2 + 1] cycloadditions, [5 + 1] cycloadditions, and other less common cycloadditions.

A review of typical biological activities of glycyrrhetinic acid and its derivatives.

Glycyrrhetinic acid, a triterpenoid compound primarily sourced from licorice root, exhibits noteworthy biological attributes, including anti-inflammatory, anti-tumor, antibacterial, antiviral, and antioxidant effects. Despite these commendable effects, its further advancement and application, especially in clinical use, have been hindered by its limited druggability, including challenges such as low solubility and bioavailability. To enhance its biological activity and pharmaceutical efficacy, numerous research studies focus on the structural modification, associated biological activity data, and underlying mechanisms of glycyrrhetinic acid and its derivatives. This review endeavors to systematically compile and organize glycyrrhetinic acid derivatives that have demonstrated outstanding biological activities over the preceding decade, delineating their molecular structures, biological effects, underlying mechanisms, and future prospects for assisting researchers in finding and designing novel glycyrrhetinic acid derivatives, foster the exploration of structure-activity relationships, and aid in the screening of potential candidate compounds.

Spatial Distribution and Estimation Model of Soil pH in Coastal Eastern China.

Soil pH is an essential indicator for assessing soil quality and soil health. In this study, based on the Chinese farmland soil survey dataset and meteorological dataset, the spatial distribution characteristics of soil pH in coastal eastern China were analyzed using kriging interpolation. The relationships between hydrothermal conditions and soil pH were explored using regression analysis with mean annual precipitation (MAP), mean annual temperature (MAT), the ratio of precipitation to temperature (P/T), and the product of precipitation and temperature (P*T) as the main explanatory variables. Based on this, a model that can rapidly estimate soil pH was established. The results showed that: (a) The spatial heterogeneity of soil pH in coastal eastern China was obvious, with the values gradually decreasing from north to south, ranging from 4.5 to 8.5; (b) soil pH was significantly correlated with all explanatory variables at the 0.01 level. In general, MAP was the main factor affecting soil pH (r = -0.7244), followed by P/T (r = -0.6007). In the regions with MAP < 800 mm, soil pH was negatively correlated with MAP (r = -0.4631) and P/T (r = -0.7041), respectively, and positively correlated with MAT (r = 0.6093) and P*T (r = 0.3951), respectively. In the regions with MAP > 800 mm, soil pH was negatively correlated with MAP (r = -0.6651), MAT (r = -0.5047), P/T (r = -0.3268), and P*T (r = -0.5808), respectively. (c) The estimation model of soil pH was: y = 23.4572 - 6.3930 × lgMAP + 0.1312 × MAT. It has been verified to have a high accuracy (r = 0.7743, p < 0.01). The mean error, the mean absolute error, and the root mean square error were 0.0450, 0.5300, and 0.7193, respectively. It provides a new path for rapid estimation of the regional soil pH, which is important for improving the management of agricultural production and slowing down soil degradation.

De Novo Synthesis of Mono- and Oligosaccharides via Dihydropyran Intermediates.

The importance of carbohydrates is evident by their essential role in all living systems. Their syntheses have attracted attention from chemists for over a century. Most chemical syntheses in this area focus on the preparation of carbohydrates from naturally occurring monosaccharides. De novo chemical synthesis of carbohydrates from feedstock starting materials has emerged as a complementary method for the preparation of diverse mono- and oligosaccharides. In this review, the history of de novo carbohydrate synthesis is briefly discussed and particular attention is given to methods that address the formation of glycosidic bonds for potential de novo synthesis of oligosaccharides. Almost all methods of this kind involve the formation of dihydropyran intermediates. Recent progress in forming dihydropyrans by Achmatowicz rearrangement, hetero-Diels-Alder cycloaddition, ring-closing metathesis, and other methods is also elaborated.

Chiral Catalyst-Directed Dynamic Kinetic Diastereoselective Acylation of Anomeric Hydroxyl Groups and a Controlled Reduction of the Glycosyl Ester Products.

A catalytic method is developed for the diastereoselective acylation of the anomeric hydroxyl group in diverse carbohydrates to form either α- or ß-anomeric esters. While exclusive formation of the ß-isomer was observed in most sugar substrates with one enantiomer of the chiral catalyst, moderate to high α-selectivity was obtained by using the other enantiomer of the chiral catalyst. The resulting α- and ß-anomeric esters have very different reactivity toward a reduction reaction.