申请人:Tanabe Seiyaku Co., Ltd.
公开号:US05703234A1
公开(公告)日:1997-12-30
Novel process for preparing azetidinone compound of the formula \x9bIII!: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula \x9bI!: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula \x9bII!: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound \x9bIll! being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.
一种制备式为\x9bIII!\的氮杂四元环化合物的新工艺:##STR1## 其中R.sup.1为H或低碳基,R.sup.2和R.sup.3与相邻的氮结合形成杂环基团,R.sup.4为保护或未保护的羟基取代的低碳基。该工艺包括将式为\x9bI!\的脂肪酰胺化合物:##STR2## 其中R.sup.1,R.sup.2和R.sup.3与上述定义相同,与式为\x9bII!\的化合物反应:##STR3## 其中L.sup.1为离去基,R.sup.4与上述定义相同,在碱存在下进行。该化合物\x9bIll!\可用作合成具有优异抗菌活性的1-甲基碳青霉烯衍生物的中间体。