Formation of C(sp2)–X bonds was carried out using a Fe3O4@SiO2‐copper(I) sucrose xanthate nanoparticle catalyst with the aid of the copper(I) xanthate moiety in the catalyst which was prepared from the reaction between sucrose and carbon disulfide through an alkaline medium via the traditional Zeise approach. Various techniques were employed for the characterization of these novel nanoparticles. Three sorts of heteroatoms, N, O and S, successfully underwent heteroatom arylation to produce secondary or tertiary amines, ethers and thioethers, respectively.
Macrocycles were designed to antagonize the protein–protein interaction p53-MDM2 based on the three-finger pharmacophore F19W23L25. The synthesis was accomplished by a rapid, one-pot synthesis of indole-based macrocycles based on Ugi macrocyclization. The reaction of 12 different α,ω-amino acids and different indole-3-carboxaldehyde derivatives afforded a unique library of macrocycles otherwise difficult to access. Screening of the library for p53-MDM2 inhibition by fluorescence polarization and 1H,15N HSQC NMR measurements confirm MDM2 binding.
In the presence of a catalytic amount of Fe3O4‐Guanidine acetic acid (GAA) nanoparticles, efficient transamidation of several amides with various amines is described under solvent‐free conditions. Fe3O4‐Guanidine acetic acid nanoparticles provide the first example of a magnetically recoverable organocatalyst for transamidation in the highest catalytic activity. The catalyst could be simply recycled with the assistance of an external magnet and reused for six runs without significant loss of its catalytic activity.
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