氟氧头孢中间体的合成工艺研究  

Study on the Synthesis of the Intermediate of Flomoxef

作　　者：贾淑艳 

机构地区：[1]哈药集团制药六厂,哈尔滨150050

出　　处：《黑龙江医药》2008年第4期57-59,共3页Heilongjiang Medicine journal

摘　　要：氟氧头孢是新型的氧头孢烯类抗生素,具有较广的抗菌谱,对革兰氏阳性菌,阴性菌、需氧菌及厌氧菌都有很强的抗菌活性。它的最大特色在于其对葡萄球菌的抗菌活性,改善了第三代头孢菌素的某些缺点。另外,它对MRSA(methicillin-resistant Staphylococcus aureous)也具有较高的抗菌活性。在临床上得到很好地运用。因此,氟氧头孢的合成研究具有重要的意义。通过对文献路线的分析,本论文选用廉价、易得的青霉素G为原料,经过氧化、开环、闭环等反应来合成氟氧头孢。现已完成中间体5(2-[2,6-二氮-4-氧-7-羰基-3-苄基]双环[3.2.0]-3 -羟甲基-3-丁烯酸二苯甲酯)的合成。并对此条合成路线进行了工艺研究和考察,确定了适合工业化生产的反应条件,其收率也较好。Flomxef is a new member of oxacephem antibiotics, having a broad spectrum and strong antimicrobial activity to G＋ , G-, aerobe and anaerobe. The most noticeable feature of flomoxef resides in its excellent antistaphylococcal activity, improving one of disadvantages of the third - generation cephalosporins. Moreover, flomoxef is highly active against most of the clinical isolates of MRSA（methicillin - resistant Staphylococcus） .Also, they have been well used in clinic. Therefore, the synthetical researches on flomoxef is greatful of significance. Based on the reported literature, by oxidation , opening , cyclization and so on, the target compound flomoxef can be obtained, we have systhaised the intermediate compound5（ diphenytmethyl 2 - [ 2, 6 - diaza - 4 - oxa - 3 - benzylbicyclo[ 3.2.0 ] hept - 6 - yl ] - 3 - hydroxymethyl - but - 3 - enoa - te） is obtained in this paper , starting from prnicillins which is low cost and can be abundantly supplied from nature.

关 键 词：氟氧头孢 氧头孢烯 中间体 工艺研究 

分 类 号：TQ465[化学工程—制药化工]