Phosphorus-containing drugs belong to an important class of therapeutic agents and are widely applied in daily clinical practices. Structurally, the phosphorus-containing drugs can be classified into phosphotriesters, phosphonates, phosphinates, phosphine oxides, phosphoric amides, bisphosphonates, phosphoric anhydrides, and others; functionally, they are often designed as prodrugs with improved selectivity and bioavailability, reduced side effects and toxicity, or biomolecule analogues with endogenous materials and antagonistic endoenzyme supplements. This review summarized the phosphorus-containing drugs currently on the market as well as a few promising molecules at clinical studies, with particular emphasis on their structural features, biological mechanism, and indications.

A general synthesis of chiral α,α-diaryl carboxamides is developed by enantioselective cross-coupling between 2bromo-2-aryl carboxamides and arylboronic acids, leading to a series of chiral α,α-diaryl carboxamides with various electronic properties and functionalities in moderate to excellent enantioselectivities and yields. The employment of a sterically bulky chiral P,PO ligand L2 is critical for the reactivity and selectivity. This protocol is applied to an efficient asymmetric synthesis of a key intermediate of dopamine receptor agonist SKF 38393. Letter pubs.acs.org/OrgLett

A new type of Atherton-Todd reaction for a convenient pseudohalogenation of phosphites has been developed. Direct azidation, cyanation, and thiocyanation of (RO) 2 P(O)H (R = Et, i-Bu, Ph) were accomplished readily with sodium pseudohalides in acetonitrile under mild modified Atherton-Todd conditions. The corresponding phosphorochloridates were demonstrated by GC/MS to be the intermediates. Pseudohalogenations of ethyl phenylphosphinate and diphenylphosphine oxide were also investigated.

Herein, we report a highly efficient and practical synthesis of chiral 2,3-dihydroquinazolinones directly from diverse aldehydesin excellent yields and enantioselectivities. This protocol affords particularly high enantiocontrol for aliphatic aldehydes (up...

Highly enantioselective rhodium-catalyzed hydrogenation of (Z)-N-sulfonyl-α-dehydroamido boronic esters is realized for the first time using a JosiPhos-type ligand. This method has enabled convenient synthesis of a series of enantio-enriched N-sulfonyl-α-amido boronic esters in good yields and excellent enantioselectivities (up to 99% ee).