Development of a green, concise synthesis of nicotinamide derivatives catalysed by Novozym® 435 from in sustainable continuous-flow microreactors.

An increasing number of studies have shown that many nicotinamide derivatives exhibited extensive biological activities, such as anti-inflammatory and antitumor activity. In this paper, a green, concise synthesis of nicotinamide derivatives in sustainable continuous-flow microreactors catalysed by Novozym® 435 from has been developed. Application of an easily obtainable and reusable lipase in the synthesis of nicotinamide derivatives from methyl nicotinate and amines/benzylamines reacted for 35 min at 50 °C led to high product yields (81.

Visible-Light-Driven -Selective Heteroarylation of -Fluoroalkyl Hydroxylamine Reagents with Quinoxalin-2(1)-ones.

Herein, we disclose a direct and powerful strategy for the synthesis of highly valuable α-trifluoromethylamine and -trifluoroethylamine derivatives from a visible-light-promoted -selective heteroarylation of -trifluoroethyl hydroxylamine reagents with quinoxalin-2(1)-ones under ambient conditions. The chemoselectivity of the process (trifluoroalkylation or -trifluoroethylamination) can easily be dictated and modulated by a selection of -trifluoroethyl hydroxylamine substrates. The key to success is the protecting group on the N atom of hydroxylamine reagents, which can control the process of 1,2-H shift of the in situ-generated trifluoroethyl radical.

Visible-Light-Promoted Xanthate-Transfer Cyclization Reactions of Unactivated Olefins under Photocatalyst- and Additive-Free Conditions.

A general visible-light-induced photocatalyst-/additive-free strategy was developed for the construction of various nitrogen-heterocycles (42 examples, up to 97% yield) such as γ-lactams, δ-lactams, pyrrolidines, indolones, quinolinones, and fused polycyclic structures at room temperature. The prominent features of this protocol are mild and environmentally friendly conditions, broad substrate scope, and good functional group tolerance. Importantly, the reaction can be performed under natural sunlight, the most sustainable energy source imaginable.