Luo You-fu
2009
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Journal
Chemistry World
Abstract
Started from L-threonine,azetidine[(3S,trans)-3-amino-4-methyl-2-oxo-1-azacyclobutylsulfonic acid] as intermediate of aztreonam was prepared via esterification,aminolysis of ester,protection of amino group by forming N-Cbz and hydroxy group by forming methanesulfonate,subsequently sulfonation on amino of amide,cyclization,and deprotection.The overall yield was 48.8%,and the purity was 98.7%(HPLC),[α]=-41°(c 1%,H_2O).The process had merits such as available raw materials,simple work-ups,highly yield and purity,and it was suitable for industrial production.