申请人:Bristol-Myers Company
公开号:US04973687A1
公开(公告)日:1990-11-27
This invention provides novel azetidinone intermediates having the formulas: ##STR1## wherein R.sup.1 is hydrogen, or a conventional hydroxy-protecting groups; R.sup.2, R.sup.4, and R.sup.5 are independently selected from the group consisting of hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; spirocycloalkyl having 3-6 carbon atoms; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; or various heterocyclic moieties; and R.sup.6 is methanesulfonyl or p-toluenesulfonyl; which are useful in the preparation of carbapenem antibiotics.
该发明提供了以下式子的新型氮杂四环酮中间体:##STR1## 其中R.sup.1是氢或传统的羟基保护基;R.sup.2、R.sup.4和R.sup.5独立地选自以下组:氢;取代和未取代的:具有1-10个碳原子的烷基,烯基和炔基;环烷基,环烷基烷基和烷基环烷基,环烷基环烷基上具有3-6个碳原子,烷基部分上具有1-6个碳原子;具有3-6个碳原子的螺环烷基;苯基;苯基烷基,苯基烯基和苯基炔基,其中芳基部分为苯基,脂肪部分具有1-6个碳原子;或各种杂环基;R.sup.6为甲磺酰基或对甲苯磺酰基。这些中间体在制备碳青霉烯类抗生素中非常有用。