(6R,7R)-7-[2-呋喃基(甲氧亚氨基)乙酰氨基]-3-羟甲基-8-氧代-5-硫杂-1-氮杂二环[420]辛-2-烯-2-甲酸的合成研究  

Study on synthesis of (6R,7R)-7-[[2-furanl(methoxyimino)acetyl]amino]-3-hydroxymethyl-8-oxo-5-thia-1-azabicyclo-3-hydroxymethyl-8-oxo-5-thia-1-azabicyclooct-2-ene-2-carboxylic acid

作　　者：赵卫良[1] 刘金庭[1] 

机构地区：[1]山东大学化学院,济南250100

出　　处：《齐鲁药事》2005年第4期237-239,共3页qilu pharmaceutical affairs

摘　　要：目的　制备(6R,7R) - 7-[2 -呋喃基(甲氧亚氨基)乙酰氨基] - 3-羟甲基- 8-氧代- 5 -硫杂- 1-氮杂二环[4 2 0]辛- 2 -烯- 2 -甲酸。方法　通过7-氨基头孢烷酸的水解,生成去乙酰基7-氨基头孢烷酸,再与2 - (2 -呋喃基)- 2 -甲氧亚胺基乙酸氯反应进行7位氨基的酰化制备上述医药中间体。结果及结论　适宜的反应条件为:7-氨基头孢烷酸在- 2 5℃水解,与2 - (2 -呋喃基) - 2 -甲氧亚胺基乙酰氯在- 10℃反应,二者的摩尔比为1 0∶1. 15,收率可达80 %。Objective To study the synthesis of (6R,7R)-7-[[2-furanl(methoxyimino)acetyl]amino]-3-hydroxymethyl-8-oxo-5-thia-1-azabicyclo-3-hydroxymethyl-8-oxo-5-thia-1-azabicyclooct-2-ene-2-carboxylic acid. Methods The objective compound can be prepared by hydrolyzed 7-anmino cephalosporanic acid under low temperature, which should then being acylated by 2-furanyl-(sin-methoxyimino)acitic chloride. Results and conclusions The suitable reaction conditions were as follows:7-amino cephalosporanic was hydrolysised at -25℃ and reacted with 2-furanyl-(sin-methoxyimino)acitic acid at -10℃.The proportion of the two materials was 1.0∶1.15 and the yield could reach 80%.

关 键 词：头孢呋辛 7-氨基头孢烷酸 水解 酰化 

分 类 号：TQ460.31[化学工程—制药化工]