Synthesis Of Amorolfine

Amorolfine is a new kind of drug for fungi with high exosomatic pharmacoactivity .Its main pharmacological action is to inhibit the reducing biocatalyst and isomerism biocatalyst needed by the procession for sub-ergotasteroid to ergosterin ,which lead to the accumulation of the sub-ergotasteroids and the reduction of the ergosterin, so damage the cell structure and fuction ,finally kill the fungus.At the same time, the deposition of abnormal chitin cased by Amorolfine hinder the ergosterin growth ,which also inhibit the activity of the NADH oxidase and reducing biocatalyst of ambercell pigment C, etc.Basing on synthesis routes exsitded,we design a new route :starting with benzene, first alkylation with tertpentanol,then acylation with propionyl chloride,subsequently,reacting with paraformaldehyde and 2,6-dimethylmorpholine,the 2-(2,6-dimethylmorpholino)-1-(4-tert- pentylphenyl) propan-1-one was obtained.finally,the objective compound was prepared bycatalytic hydrogenation at the presence of Pd/C.this route is very feasible with fewer steps ,cheaper material and higher yield .