Synthesis Of Phenoxyacetamide Derivatives

As an important chemical raw material,phenoxyacetamides are the basic structural unit of many drugs and have a wide range of biological activities,such as antibacterial,anticancer,tyrosinase inhibition,weeding,and sterilization.As an intermediate for many drug synthesis,it contains amide groups that not only constitute multi-functional components in synthetic organic chemistry,but also have wide applications in the design of lead compounds and the synthesis of drugs,so it is convenient,efficient and green.The synthesis of such compounds is of great significance.In this paper,a new"one-pot"method for synthesizing phenoxyacetamides was established.The green solvent"water"was used as the reaction solvent and the green oxidant"H₂O₂"was used as the reaction oxidant to introduce the green pharmaceutical concept into phenoxylate.The synthesis of amide drug lead compounds.In the process of establishing the mode reaction of bromoacetonitrile and phenylboronic acid,the effects of alkali,temperature and time on the reaction were investigated by using bromoacetonitrile and phenylboronic acid as substrates.The results showed that without catalyst,1.3 mmol NaOH was used as the base,pure water was used as the solvent,30%H₂O₂ 0.08 mL was added,and 80 ^oC was heated for 4 h.The isolated yield of phenoxyacetamide was 76%.Under this condition,a total of 25 of phenoxyacetamide derivatives were synthesized,especially derivatives with sensitive groups.The broad applicability of this system to the synthesis of phenoxyacetamide substrates was evaluated.In summary,through the research of this subject,the defects in the synthesis of phenoxyacetamide derivatives have been effectively solved:if the reaction conditions of traditional synthetic methods severely limit the synthesis of derivatives containing sensitive groups,it is usually necessary to adopt toxic,The flammable and volatile organic solvent and the further hydrolysis of the cyano group to the carboxylic acid are difficult to effectively suppress;although the transition metal catalysis method has made great progress,the precious metal catalyst is difficult to synthesize,expensive,and the product and the catalyst are difficult to separate,which limits its Application in large-scale industrial production.This research work fully embodies the concept of green pharmaceuticals.The superiority of this strategy step economy,as well as the environmentally friendly solvent system,has shown broad application prospects for its industrial development.