a b s t r a c tSulfur (S VI ) based moieties, especially, the sulfonyl or sulfonamide based analogues have showed a variety of pharmacological properties, and its derivatives propose a high degree of structural diversity that has established useful for the finding of new therapeutic agents. The developments of new less toxic, low cost and highly active sulfonamides containing analogues are hot research topics in medicinal chemistry. Currently, more than 150 FDA approved Sulfur (S VI )-based drugs are available in the market, and they are widely used to treat various types of diseases with therapeutic power. This comprehensive review highlights the recent developments of sulfonyl or sulfonamides based compounds in huge range of therapeutic applications such as antimicrobial, anti-inflammatory, antiviral, anticonvulsant, antitubercular, antidiabetic, antileishmanial, carbonic anhydrase, antimalarial, anticancer and other medicinal agents. We believe that, this review article is useful to inspire new ideas for structural design and developments of less toxic and powerful Sulfur (S VI ) based drugs against the numerous death-causing diseases.

A method of SO2F2 mediated direct clickable coupling of carboxylic acids with amines for the synthesis of a broad scope of amides and peptides was developed.

A review of recent developments in the synthesis and biological applications of arylnaphthalene lactones analogs.

A clickable connective hub 1-bromo-2-triazolethane-1-sulfonyl fluoride BTESF (1) was developed and successfully applied for the fluorosulfonylvinylation of a host of primary and secondary cyclic or acyclic amines including amino acids and pharmaceuticals. Further antimicrobial experiments revealed that vinyl sulfonyl fluoride functionalized norfloxacin (3ak), ciprofloxacin (3am), and lomefloxacin (3an) exhibited 4-fold improved antimicrobial activity against Gram-positive bacteria compared to their parent drugs.

A SO2F2 mediated Pd-catalyzed one-pot dehydroxylative cyanation of phenols to aryl nitriles was accomplished by employing (K4[Fe(CN)6]) as the cyanating reagent.

The construction of (Z)‐(hetero)arylethenesulfonyl fluorides was achieved utilizing Iridium photoredox catalysis under UV‐light irradiation. This protocol provided a diverse range of (Z)‐(hetero)arylethenesulfonyl fluorides in moderate to good yields under mild conditions without external additives. The late‐stage transformation of the (Z)‐(hetero)arylethenesulfonyl fluorides comparing with their E‐configuration counterparts was also studied.

A practical Pd‐catalyzed direct dehydroxylative coupling of (hetero)benzylic alcohols with (hetero)arylboronic acids for the constructions of di(hetero)arylmethane derivatives under SO2F2 was described. This new method provided a strategically distinct approach to di(hetero)arylmethane derivatives from readily available and abundant benzylic alcohols under mild condition.

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