The Technology Research In Total Synthesis Of Antimiaobial Agent Lenampicilin

In this paper, A method for preparation of lenampicilin hydrochloride was reported.3-hydroxy-2-butanone as raw material was treated with triphosgene through a series of reactions including acylation,cyclization and dehydrochlorination to give 4,5-dimethyl- 1,3-dixolene-2-one( DMDO) . And then DMDO was chloridated with sulfonyl chloride and further rearranged giving DMDO-C1.Lenampicilin hydrochloride was prepared from DMD0-C1 and aminobenzopenicillin via esterification.The tolal yield of lenampicilin hydrochloride was 37%. Structures of the intermediates and lenampicilin hydrochloride were characterized by IR and 1HNMR. The systhesizing method had the advantages such as the simple reaction steps and easy operation. It is an attempt to set up a foundation of industry production of lenampicilin...