Research On The Synthesis Of Furan Derivatives With Various Biological Activity

The five-membered heterocyclic structure is an important functional group of many bioactive substances.The furan heterocycle is particularly prominent in this respect.The furan heterocycle is a common functional group or even a nucleus in various drugs.For example,it has analgesic and anti-?-opioid receptor agonist Salvadoran B,?-lactam antibiotics,three generations of cephalosporins cefuroxime and so on.The synthesis of various furan analogs under basic conditions using ?-haloketones and ?-dicarbonyl compounds is the most common synthesis method.But the academic community for this reaction to replace the site has been controversial,so our task group for this issue to do the following:1.the chemical selectivity of the reaction results:a)Some scholars believe that the reaction site is located in the ?-halogenated ketone halogenated carbon,the occurrence of SN2 substitution reaction to form tricarbonyl compounds.The resulting product was subjected to Paal-Knorr reaction to give furan.b)Some scholars believe that the reaction site in the ?-haloketone carbonyl carbon,the first occurrence of aldol condensation reaction,and then through the molecular alkylation of dihydrofuran,the intermediate is easy to dehydrate the formation of furan,Which is the Feist-Bénary reaction.2.A method for the selective synthesis of tricarbonyl compounds or dihydrofuran has been found.3.we found a new reaction conditions: ?-halogenated ketone and ?-dicarbonyl compounds in the absence of alkali and solvent conditions,direct heating reaction to obtain furan derivatives.