📜莫西沙星置于sodium Cyanide体系中,用 二甲基亚砜 用作溶剂,化学反应 17.0H,以99%的收率获得莫西沙星去羧基类似物
参考文献:Synthesis And Evaluation Of 1-Cyclopropyl-2-Thioalkyl-8-Methoxy Fluoroquinolones
标题:Synthesis And Evaluation Of 1-Cyclopropyl-2-Thioalkyl-8-Methoxy Fluoroquinolones
摘要:Novel Fluoroquinolone Derivatives Substituted With A 2-Thioalkyl Moiety,With And Without A Concomitant 3-Carboxylate Group,Were Synthesized To Evaluate The Effect Of C-2 Thioalkyl Substituents On Gyrase Binding And Inhibition. The Presence Of A 2-Thioalkyl Group Universally Decreased Activity As Compared To Parent Fluoroquinolones. However,With Derivatives Of Moxifloxacin The Presence Of Either A 2-Thioalkyl Group Or A 3-Carboxylate Moiety Increased Activity Over The 2,3-Unsubstituted Derivative. Energy Minimization Of Structures Provides An Explanation For Relative Activities Of Fluoroquinolones Having A C-2 Thio Moiety. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.05.112