申请人:Eli Lilly and Company
公开号:US04368156A1
公开(公告)日:1983-01-11
Process for 4-halo azetidinones of the formula ##STR1## wherein R.sub.1 is acylamino or diacylamino, X is chloro, bromo or iodo, and R is a carboxy-protecting group which comprises treating a 4-sulfinoazetidinone of the formula ##STR2## with positive halogen reagent, eg. N-chlorosuccinimide, N-bromosuccinimide, N-iodosuccinimide, hypohalite. The 4-haloazetidinones are useful intermediate for .beta.-lactam antibiotics.
公式为 ##STR1## 其中R.sub.1为酰胺基或二酰胺基,X为氯、溴或碘,R为羧酸保护基的4-卤代氮杂环戊酮的制备方法包括用正卤素试剂(例如N-氯代琥珀酰亚胺、N-溴代琥珀酰亚胺、N-碘代琥珀酰亚胺、次卤酸盐)处理公式为 ##STR2## 的4-亚磺酰基氮杂环戊酮。4-卤代氮杂环戊酮是β-内酰胺类抗生素的有用中间体。