The development of regioselective aldol reactions of β-methyl-substituted cyclic enone derivatives with isatins to afford the aldol products with the bond formation at the methyl group of the β-methyl-substituted cyclic enone derivatives is described. Catalyst systems composed of DBU and pyrrolidine with DMSO were identified that resulted in the aldol reactions with almost perfect regioselectivities. DBU, pyrrolidine, and DMSO were all required to selectively afford the γ-position-reacted aldol products. With the use of this method, the scope of the 3-substituted 3-hydroxyoxindole derivatives ..read more

Amides are important compounds in organic synthesis and have significant roles in pharmaceuticals, agrochemicals, and materials. The Ritter reaction is a classical transformation to amides between nitriles and alcohol derivatives or olefins. para-Quinone methides (p-QMs) are highly reactive intermediates in organic synthesis. The cover picture visualizes that, as new Ritter acceptors, para-quinone methides are joining the alcohols and alkenes, known Ritter acceptors, driving to amides. More information can be found in the Research Article by Nurullah Saracoglu et al ..read more

Peptide-phosphonium salt (PPS) catalysts, which contain multiple hydrogen-bonding donors, have displayed remarkable phase-transfer catalytic efficiency in recent years. The cover art demonstrated that PPS catalysts can efficiently promote the enantioselective Mannich/radical debromination cascade of α-brominated ketones with pyrazolinone ketimines to access valuable chiral β-amino ketone-pyrazolinone scaffolds. This protocol would open new avenues for organocatalytic enantioselective radical reactions. More information can be found in the Research Article by Tianli Wang et al ..read more

Herein, we report a simple and straightforward magnetic heterogeneous catalytic (Ni@C) approach to synthesize benzimidazole and quinoxaline scaffolds from o-phenylene diamines with primary amines using H2O as an environmentally benign solvent. The Ni@C catalyst was synthesized using a pyrolysis method and unambiguously analyzed by various characterization techniques. The scope of the catalytic methodology was presented with various o-phenylene diamines and primary amines producing a range of benzimidazoles and quinoxalines in good to excellent yields. The notable feature include reusability of ..read more

This article describes the development of a metal and additive-free protocol that utilizes acetic acid (AcOH) as a catalyst for the C3-alkylation of indolizines using para-Quinone Methides (p-QMs) as an alkylation agent. The metal and additive free method offers an easy route to various substituted indolizine derivatives with good functional group tolerance and delivering acceptable good yields (up to 93%). A gram-scale synthesis and further product derivatization show the synthetic potential of this technique. The significance of these findings for medicinal chemistry makes this easy and gree ..read more

Herein we report an improved self-assembling phosphorus ligand based on hydrogen bonding between pyridone/hydroxypyridine in the ligand backbone. The N-pyrrolyl substituents significantly improve the π-backbonding properties of the ligand. Rhodium, iridium and platinum complexes of the ligand were prepared and analyzed by NMR spectroscopy and x-ray crystal structure analysis. A catalyst based on this ligand showed very high catalytic activity and linear regioselectivity in rhodium-catalyzed hydroformylation of 1-octene. The same ligand was applied in linear regioselective iridium-catalyzed hyd ..read more

C−S bond formation has attracted considerable interest for a long time. The cover picture shows a straightforward and efficient C−S bond formation reaction via S−H insertion of phosphorodithioic acids with diazo compounds under catalyst-, and light-free conditions. It provides a simple strategy for the construction of C−S bond with high atom economy and allows access to some marketed phosphorodithioate pesticides, candidate agrochemicals and other interesting sulfur-containing molecules. More information can be found in the Research Article by Ming-Hua Xu et al ..read more

Photocatalytic generation of alkoxy radicals is fast emerging as an essential method for the generation of diverse and valuable inert carbon radicals for the construction of various C(sp3)–C(sp3), C(sp3)–C(sp2), C(sp3)–C(sp), and C– heteroatom bonds under mild condition. This review is a comprehensive evaluation of the studies using N-alkoxyphthalimides (NAPI) derivatives as tunable oxygen radical precursors in photoredox catalysis, highlighting alkoxy radical enabled 1,2-, 1,5hydrogen atom transfer, and β-fragmentation (deformylation) process to generate versatile carbon-centered radical inte ..read more

We have developed a Lewis base–silyl Lewis acid cooperative catalyst for the iodochlorination of alkenes. In the presence of 10–20 mol% of Ph3P=O, the iodochlorination of tetrasubstituted alkenes with N-iodosuccinimide and tert-butyldimethylchlorosilane proceeded efficiently at –40 °C to provide the corresponding 1,2-iodochloroalkanes that cannot be easily obtained via conventional methods. A series of 31P NMR experiments suggests that the cooperative activation of the reaction components facilitates the generation of the active iodochlorinating species ..read more

Amines are widely applied in the chemical and pharmaceutical industries, and the development of synthetic methods for their preparation is driven by their importance. The amination of alkenes is a direct and efficient method for the construction of amines, of which oxidative amination is more valuable because it can give the desired products with greater functionality and flexibility. In oxidative amination, using molecular oxygen (O2) as a terminal oxidant has promising industrial application prospects. In recent years, the palladium-catalyzed ..read more