摘要
设计并成功建立了以7-苯乙酰氨基-3-氯甲基-4-头孢烷酸对甲氧基苄酯(GCLE)为原料合成7-氨基-3-乙烯基头孢烷酸(7-AVCA)的路线,并对其工艺条件进行了优化,确定了7-AVCA的最佳合成条件.当n(GCLE)∶n(PPh3)∶n(NaI)∶n(HCHO)∶n(NaOH)为1.0∶1.1∶1.0∶10.6∶0.976时,3-乙烯基头孢菌素中间体5的收率为90.7%;当n(中间体5)∶n(苯酚)为1.0∶10.0,反应温度为60℃,反应时间为4 h时,7-AVCA的收率为77.0%.
The synthetic route of 7-AVCA from GCLE was designed and successfully established in this paper.The reaction conditions were optimized and confirmed.The yield of 3-vinylcephem intermediate 5 was 90.7% while the ratio of n（GCLE）∶n（PPh3）∶n（NaI）∶ n（HCHO）∶n（NaOH） was 1.0∶1.1∶1.0∶10.6∶0.976.The yield of 7-AVCA was 77.0% while the ratio of n（3-vinylcephem intermediate 5）∶n（phenol） was 1.0∶10.0,the temperature was 60 ℃ and the reaction time was 4 h.
出处
《河北大学学报（自然科学版）》
CAS
北大核心
2010年第4期375-380,共6页
Journal of Hebei University(Natural Science Edition)
基金
国家自然科学基金资助项目(20806018)
河北省教育厅自然科学研究重点计划资助项目(ZD200910)
