We used a readily available water source, MgSO4·2H2O, to realize the control of the chemo-selectivity of the Ritter-type reaction efficiently.

Chemo-selective control of Ritter-type reaction by coordinatively unsaturated inorganic salt hydrates

Synergistic detoxification by combined reagents and safe filling utilization of cyanide tailings

C(3)-Aminoisoindolinones have attracted the attention of medicinal chemists due to their unique and stable N−C−N substructure and possibilities for facile and scalable synthesis of combinatorial libraries. We discovered that para-toluenesulfonic acid (PTSA), an organic protic acid, efficiently catalyzes condensation of isoindolinone-3-ols with primary and secondary amines to furnish C(3) N-substituted isoindolinones in high yields. The N−C bond formation reaction is highly efficient and experimentally simple. The method replaces known transition metal catalysts involving Cu, Pt, Pd or Au. It works efficiently for both intra- and inter-molecular variants. Furthermore, it is amenable for synthesis of C(3)-aminoisoindolinones with free N(2) via photolytic deprotection of the 2-nitrobenzyl group. We have demonstrated application of the method for synthesis of a variety of medicinally relevant bicyclic and tricyclic C(3)-aminoisoindolinones. 

Facile and High‐Yielding Synthesis of C(3)‐Aminoisoindolinones Under Metal Catalyst‐Free Conditions

We have developed a straightforward electrochemical protocol for direct α-amidation and α-pyrazolation of N-alkoxy- and N-aryloxycarbonyl pyrrolidines with amides or pyrazoles. Unlike previously reported methods, this protocol does not require...

Electrochemical Direct α-Amidation and α-Pyrazolation of N-Alkoxy- and N-aryloxycarbonyl Pyrrolidines

Synergistic detoxification by combined reagents and safe filling utilization of cyanide tailings.

Isoindolinones are ubiquitous structural motifs in natural products and pharmaceuticals. Establishing an efficient method for structural modification of isoindolinones could significantly facilitate new drug development. Herein, we describe copper-promoted direct amidation of isoindolinone scaffolds mediated by sodium persulfate. The method exhibits mild reaction conditions and high site-selectivity, and enables the structural modification of the drug indobufen ester with various amides with yields of 49 to 98%. It is also gram-scalable. Additionally, the reaction mechanism appears to involve a radical and a carbocationic pathway.

Copper-promoted direct amidation of isoindolinone scaffolds by sodium persulfate

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Copper-promoted direct amidation of isoindolinone scaffolds by sodium persulfate