P-Alkylation Of N-Aryl Phosphinecarboxamides And Synthesis Of Disubstituted Hypophosphite

Organophosphorus compounds are closely related to people's lives,and they have a wide range of applications in the fields of catalysis,materials,and medicine.In2013,the phosphorous urea of the urea analogue has been synthesized from the phosphorus phosphonate anions.Since then,the synthesis of phosphorous urea and its derivatives has attracted great research interest.At the same time,functionalized,differentiallysubstitutedphosphinateestersR₁R₂P?O??OR?areimportant organophosphorus intermediates,particularly in the synthesis of medicinally relevant protease inhibitors and ATP-dependent ligases.Therefore,the synthesis of disubstituted hypophosphites and phosphorous urea derivatives have important research significance.In this dissertation,the synthesis of phosphocarboxamides and disubstituted hypophosphites was reviewed.On this basis,the nucleophilic reactivity of N-arylphosphocarboxamidesandthealkoxylationoxidationof alkyl-N-phenylphosphanecarboxamides were explored and designed.The specific work during the master's degree is as follows:1.Using Cs₂CO₃ as the base and DMSO as a solvent,the P-alkylation of N-arylphosphocarboxamides with various haloalkanes was realized at room temperature.A series of alkyl-N-phenylphosphanecarboxamides were synthesized.At the same time,it was also found that N-arylphosphocarboxamides can not only be used as nucleophilic reagents for P-alkylation reaction,but also the carbonyl sites of N-arylphosphocarboxamides could be added-eliminated by some nucleophilic reagents such as morpholine,phenylthiophenol and diphenyl disulfide.2.Using the above products as a raw material and I₂ as an additive,a series of carbamoylalkylhypophosphites are synthesized by the alkoxylation and oxidation reaction of P-H with alcohols in a short time at room temperature.