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Relevant academic research and scientific papers

Regioselective C-H Thioarylation of Electron-Rich Arenes by Iron(III) Triflimide Catalysis

A mild and regioselective method for the preparation of unsymmetrical biaryl sulfides using iron(III) catalysis is described. Activation of N-(arylthio)succinimides using the powerful Lewis acid iron(III) triflimide allowed the efficient thiolation of a range of arenes, including anisoles, phenols, acetanilides, and N-heterocycles. The method was applicable for the late-stage thiolation of tyrosine and tryptophan derivatives and was used as the key step for the synthesis of pharmaceutically relevant biaryl sulfur-containing compounds such as the antibiotic dapsone and the antidepressant vortioxetine. Kinetic studies revealed that while N-(arylthio)succinimides bearing electron-deficient arenes underwent thioarylation catalyzed entirely by iron(III) triflimide, N-(arylthio)succinimides with electron-rich arenes displayed an autocatalytic mechanism promoted by the Lewis basic product.

Metal- And solvent-free direct C-H thiolation of aromatic compounds with sulfonyl chlorides

A simple, efficient and green method for the direct thiolation of aromatic compounds using commercially available sulfonyl chlorides as the sulfur source was developed under metal- and solvent-free conditions. The C-S bond was constructed via direct C-H functionalization of diverse aromatic compounds under an oxygen atmosphere. In this process, various diaryl sulfides were synthesized in moderate to excellent yields. This protocol shows a broad substrate scope and good functional group tolerance. Moreover, a gram-scale experiment was also conducted to prove the prospect of this method for the scale-up synthesis of diaryl sulfides. Mechanistic studies indicate that this procedure probably undergoes a radical pathway.

Metal-free C-H thioarylation of arenes using sulfoxides: A direct, general diaryl sulfide synthesis

Metal-free C-H thioarylation of arenes and heteroarenes using methyl sulfoxides constitutes a general protocol for the synthesis of high value diaryl sulfides. The coupling of arenes and heteroarenes with in situ activated sulfoxides is regioselective, uses readily available starting materials, is operationally simple, and tolerates a wide range of functional groups.

Design, synthesis, and structure - Activity relationship of N-arylnaphthylamine derivatives as amyloid aggregation inhibitors

Dyes like CR are able to inhibit the aggregation of Aβ fibrils. Thus, a screening of a series of dyes including ABBB (1) was performed. Its main component 2 tested in an in vitro assay (i.e., ThT assay) showed good potency at inhibiting fibrils associatio

NAPHTHYL DERIVATIVES INHIBITORS OF THE BETA-AMYLOID AGGREGATION

Compounds useful in the treatment of disorders characterised by deposits of amyloid aggregates are herein described together with pharmaceutical compounds containing the same. In particular the compounds of the present invention are those having the Formula (I) as reported below. where the radicals have the meaning indicated in the description.