Microchip Based Isolation and Drug Delivery of Patient-Derived Extracellular Vesicles Against Their Homologous Tumor.

Extracellular vesicles (EVs) have demonstrated significant potential in drug delivery and anti-tumor therapy. Despite this promising strategy, challenges such as specific targeting, EVs purification persist. In this study, a personalized nanodrug delivery platform using patient-derived tumor EVs (PT-EVs) based on a microchip is presented.

Gold-catalyzed synthesis of oxazoles from alkynyl triazenes and dioxazoles.

A gold-catalyzed regioselective [3 + 2] cycloaddition of alkynyl triazenes with 1,2,4-dioxazoles was developed. The triazene group in the products could be replaced to obtain iodo-oxazoles, providing potential transformations to diverse oxazole structures. This protocol features readily available starting materials, mild reaction conditions and scalability.

Metathesis Reaction of Diazo Compounds and para-Quinone Methides for C-C Double Bond Formation: Synthesis of Tetrasubstituted Alkenes and Quinolinones.

The para-quinone methides (p-QMs) are activated by Lewis acid and then attacked by diazo compounds. The following rearrangement leads to nitrogen gas extrusion and C-C double bond formation to constitute a metathesis reaction process. Therefore, the diazoester is transformed into tetrasubstituted alkenes, whereas the diazo-oxindole delivers the quinolinone products.

Rh(iii)-catalyzed C-H activation/cyclization of oximes with alkenes for regioselective synthesis of isoquinolines.

A Rh(iii)-catalyzed C-H activation/cyclization of oximes and alkenes for facile and regioselective access to isoquinolines has been developed. This protocol features mild reaction conditions and easily accessible starting materials, and has been applied to the concise synthesis of moxaverine. A kinetic isotope effect study was conducted and a plausible mechanism was proposed.

Fe-Catalyzed Hydroalkylation of Olefins with para-Quinone Methides.

A novel Fe-catalyzed hydroalkylation of olefins with para-quinone methides (p-QMs) for accessing phenols has been developed. In this protocol, various olefins could convert to alkyl radicals and undergo addition to para-quinone methides toward C-C bond formation and aromatization. The reaction conditions are mild and the substrate scopes are broad.

Triply Hydrogen-Bond-Directed Enantioselective Assembly of Pyrrolobenzo-1,4-diazine Skeletons with Quaternary Stereocenters.

Highly efficient synthesis of optically enriched pyrrolobenzo-1,4-diazines bearing quaternary stereocenters has been realized through the chiral Brønsted acid-catalyzed Pictet-Spengler reaction of 2-(1H-pyrrol-1-yl)anilines and α-ketoamides in good to excellent yields and enantioselectivities. Computational studies suggest an unprecedented phenomenon whereby the chiral phosphoric acid catalyst employs attractive arene C-H⋅⋅⋅N hydrogen bonding to activate the substrate and induce chirality through a triple hydrogen-bonding interaction.

Organocatalytic asymmetric multicomponent reactions of aromatic aldehydes and anilines with β-ketoesters: facile and atom-economical access to chiral tetrahydropyridines.

The first catalytic asymmetric pseudo five-component (AB(2)C(2) type) reaction is reported. A spirocyclic chiral phosphoric acid catalyzed one-pot multicomponent reaction of aromatic aldehydes, anilines and β-ketoesters and afforded highly functionalized enantioenriched tetrahydropyridines with high levels of stereocontrol.

A general access to 1,1-cyclopropane aminoketones and their conversion into 2-benzoyl quinolines.

1,1-Cyclopropane aminoketones were efficiently synthesized in high yields by the tandem reaction of α-amino aryl ketones with vinyl sulfonium salts using DBU as the base in CH(2)Cl(2). This methodology was utilized to synthesize 2-benzoyl quinolines.

A straightforward one-pot multicomponent synthesis of polysubstituted pyrroles.

Polysubstituted pyrroles were efficiently synthesized in moderate yields by a one-pot multicomponent reaction starting from primary amines, ethyl glyoxalate and 2-bromoacetophenones in the presence of pyridine in refluxing acetonitrile. This methodology was utilized to synthesize a highly substituted benz[g]indole.