摘要
本文对 3α -甲基 - 7-氧代 - 3β - ( 1H - 1 ,2 ,3-三唑 - 1 -甲基 ) - 4-硫杂 - 1-氮杂双环 [3,2 ,0 ]庚烷 - 2α -羧酸 - 4,4 -二氧化物 (他唑巴坦 )的合成进行了研究 ,尤其对其中的氯化环合和叠氮化两步反应的影响因素进行了系统研究。试验以6 -APA为原料 ,经重氮化溴化、氧化、氯化环合等 1 1步反应 ,最终得到了 4
The synthesis of 3α-methyl-7-oxo-3β-(1H-1,2,3 triazol-1-ylmethyl)-4-thia-azobicyelo[3,2,0] heptane 2α-carboxylic acid-4,4-dioxide(tazobactam) was studied in this paper, particularly the affecting factors of the chlorization cyclization and azide substitution. The synthesis of tazobactam was described starting with 6-aminopenicillanic acid in eleven steps, that include diazotization-bromination, oxidation, chlorization cyclization and so on. Finally tazobactam was obtained and the total yield was about 4%.
出处
《化学工业与工程》
CAS
2002年第3期219-224,273,共7页
Chemical Industry and Engineering
基金
天津市自然科学基金资助项目 (0 0 36 0 1811)
关键词
他唑巴坦
Β-内酰胺酶抑制剂
6-APA
氯化环合
叠氮化
tazobactam
β-lactamase inhibitor
6-aminopenicillanic acid
chlorization cyclization
azide substitution
