Dimephosphone analogs: a pharmacological aspect

“On‐Water” Synthesis of Sterically Congested γ‐Ketophosphine Oxides Featuring a CF3‐ and P(O)‐Tetrasubstituted Carbon Center

“…For example, (4‐amino‐3‐oxopentyl)phosphonic acid ( I ) and its analogs are effective D‐alanine‐D‐alanine ligase inhibitors [2a] . Dimephosphone ( II ) is one of the first organophosphorus drugs that has been used since 1983 as an antiacidotic agent and vasoactive agent [2c–d] . Over the past decades, these frameworks have garnered considerable attention, leading to intense research efforts aimed at developing efficient synthetic approaches to access them [3–12] …”

An efficient direct phosphinylation and alkylation of ketones to construct C–P and C–C bonds: access to α,α-disubstituted γ-ketophosphine oxides

“…8 Moreover, 4-(diethylphosphoryl)-4-methylpentan-2-one, one of the first γ-ketophosphine oxide drug precursors, has demonstrated high anticholinesterase activity upon further transformation (Scheme 2). 9 However, the synthesis of the anticholinesterase skeleton required multiple steps or complex available substrates in previous reports, 10 and our strategy can be performed in only one step with easily available substrates of ketones (Scheme 2). As a result of the interest in the biological activity of γ-ketophosphine oxides, intense research has been conducted on synthesis strategies for the preparation of this structural motif.…”

9-BBN and chloride catalyzed reduction of chlorophosphines to phosphines and diphosphines

“…Organophosphorus compounds are employed in numerous applications including optoelectronic materials, 1 pharmaceuticals, 2,3 and of course as ligands in transition metal chemistry. 4 The synthesis of compounds containing such fragments is often based on nucleophilic reactions with chlorophosphines (R 2 PCl) or the generation of a phosphorus based nucleophile by deprotonation of secondary phosphines (R 2 PH).…”