Electrochemically promoted thio-Michael addition of -substituted maleimides to thiols in an aqueous medium.

A stable and practical electrochemical method was developed to promote the thio-Michael addition of -substituted maleimides to various thiols in an aqueous medium. This protocol was found to be excellent in terms of facile scale-up, oxidant- and catalyst-free conditions, broad substrate scopes, good functional group tolerance, and easily available substrates. Notably, a plausible reaction mechanism was derived from the results of a series of control experiments and CV studies, which indicated that a radical pathway might speed up the thio-Michael addition under constant current.

Catalyst-free electrochemical sulfonylation of amines with sulfonyl hydrazide in aqueous medium.

An efficient electrochemical sulfonylation of amines with sulfonyl hydrazides under exogenous-oxidant-free and catalyst-free conditions in aqueous medium was developed. A wide variety of sulfonamides were prepared a simple electrochemical process from various cyclic or acyclic secondary amines, as well as more challenging free primary amines with equivalent amount of aryl/heteroaryl hydrazides in air under mild conditions. This protocol was found to be excellent in terms of facile scale-up, and to show great potential in the modification/synthesis of bioactive compounds.

Design, synthesis and mechanism study of novel natural-derived isoquinoline derivatives as antifungal agents.

In screening for natural fungicidal leads, two series of novel 3-aryl-isoquinoline derivatives 8 and 9 were designed and synthesized based on sanguinarine, chelerythrine and berberine. Their structures were confirmed by 1D, 2D NMR and HRMS. Most of the title compounds showed medium to excellent antifungal activity in vitro at 50 mg/L, which were much more active than the lead of sanguinarine.