摘要
以吡啶-2,3-二羧酸为原料,依次经脱水、氨解、环合、还原吡啶环及羰基、拆分和氢解脱苄基得(S,S)-八氢-6H-吡咯并[3,4-b]吡啶后,与1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代喹啉-3-羧酸根-硼-二乙酸酐缩合并水解去螯合得到莫西沙星。总收率43.3%。
Moxifloxacin was synthesized from pyridine-2,3-dicarboxylic acid via dehydration, benzylamination,cyclization, reduction of pyridine ring and carbonyl groups, resolution and debenzylation to afford (S,S)-octahydro-6H-pyrrolo[3,4-b]pyridine which condensed with the boric chelate of the quinolone intermediate and then hydrolysis with anoverall yield of 43.3%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2004年第3期129-131,共3页
Chinese Journal of Pharmaceuticals
关键词
莫西沙星
合成
氟喹诺酮
抗菌剂
moxifloxacin
fluoroquinolone
antibacterial agent
synthesis
