Efficient Amidation and Esterification of Phosphoric Acid Using Cl₃CCN/ Ph₃P

We developed a simple, convenient, one-pot synthetic method to synthesize phosphoramides and phosphates. This protocol has many attractive features, such as mild reaction conditions, short reaction times, and operational simplicity. In organophosphorous chemistry, phosphoryl amides and esters are important due to their broad ranges of biological properties and presence in bioactive molecules, such as natural products, amino acid analogues, pharmacological agents, and synthetic precursors. These phosphate motifs are often used as prodrugs to enhance the water solubility or therapeutic potential of parent drugs. Phosphoramides play significant roles in modern organic chemistry, as they can be used in enantioselective catalytic processes that are activated by Lewis bases, including aldol additions and allylation reactions. An important use of dialkyl, dibenzyl, and diphenyl phosphoramidates is protecting amino groups. Phosphoric acid esters are among the most valuable substances in material and medicinal chemistry. Owing to their widespread use, general and convenient access to these compounds is desirable