摘要
目的合成抗生素替加环素并改进其合成工艺。方法以米诺环素为起始原料,经过对其9位进行硝化,还原得到9-氨基米诺环素盐酸盐,再与叔丁基甘氨酰氯盐酸盐缩合制得替加环素。结果所得产物经过LC-MS谱,核磁共振谱等确证了结构。结论改进后的工艺路线短,杂质数量少,C-4差向异构体含量小,成本低,污染小,适合大规模生产。
Objective To improve the synthesis of tigecycline. Methods The tigecycline was preparated by a three-step procedure from minocycline. Firstly, minocycline was converted to the intermediate 9-nitro-minocycline by nitration. Then 9-nitro-minocycline was reduced to 9-amino-minocycline, followed by condensation with the N-t- Butylglycine acid chloride hydrochloride. Results Chemical stucture of tigecycline was confirmed by ＂LC-MS, 1H-NMR, etc.. Conclusion A more reasonable operational path for the manufacturing process of tigecycline has been developed.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2013年第12期918-920,927,共4页
Chinese Journal of Antibiotics
关键词
替加环素
合成
抗生素
Tigecycline
Synthesis
Antibiotic
