头孢罗宁的合成  

Synthesis of cephalonium

作　　者：李江红[1] 石克金[1] 陈林[1] 赵俊[1] 杜伟宏[1] 曹胜华[1] 

机构地区：[1]成都大学四川抗菌素工业研究所,成都610052

出　　处：《中国抗生素杂志》2015年第7期513-515,共3页Chinese Journal of Antibiotics

摘　　要：目的合成头孢罗宁。方法 7-ACA与异烟酰胺反应得到7-氨基-3-[(4-氨基甲酰吡啶-1-基)甲基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸(简写:7-PACA),再与2-噻吩乙酰氯反应得到终产物头孢罗宁。结果总收率23.4%,产品质量符合英国药典(兽药)标准。结论本工艺易操作,为中试生产提供了依据。Objective To synthesize cephalonium. Methods 7-ACA reacted with isonicotinamide to afford 7-amino-3-（4-carbamoyl pyridinium-1-ylmethyl）-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid（7- PACA）, followed by condensation with 2-thiopheneacetyl chloride to obtain cephalonium. Results The overall yield was 23.4%. The product complies with British Pharmacopoeia （Veterinary） specification. Conclusion This process was prone to operate and provided a basis for mass production scale.

关 键 词：头孢罗宁 异烟酰胺 2-噻吩乙酰氯 

分 类 号：R978.11[医药卫生—药品]