摘要
以头孢他啶侧链酸(ATTBA)为原料,首次采用酰氯法制备氨曲南,即在双(三氯甲基)碳酸酯(BTC)/三苯基氧膦(TPPO)体系作用下,现场制备酰氯盐酸盐中间体,再与trans-3(S)-氨基-4-甲基-2-氧代-1-氮杂环丁烷基磺酸反应,最后脱保护得氨曲南,总收率为40.6%。
A new access to aztreonam was firstly developed through transformation of ceftazidime side chain （ATFBA） into its carbonyl chloride intermediate with the aid of bis（trichloromethyl）carbonate （BTC） and triphenylphosphine oxide （TPPO） system. Then this key intermediate was readily reacted with trans-3 （S）- amino-4-methyl-2-oxo-1-azetidinesulfonic acid, followed by deprotection of t-butyl group to afford aztreonam with the overall yield of 40.6%.
出处
《浙江化工》
CAS
2013年第7期10-13,共4页
Zhejiang Chemical Industry
关键词
氨曲南
双(三氯甲基)碳酸酯
三苯基氧膦
酰氯法
aztreonam
bis（trichloromethyl）carbonate
triphenylphosphine oxide
carbonyl chloride
