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Three-Component One-Pot Approach to Highly Efficient and Sustainable Synthesis of the Functionalized Quinolones via Linear/Branched Domino Protocols, Key Synthetic Methods for the Floxacin of Quinolone Drugs
ACS Omega ( IF 3.7 ) Pub Date : 2018-09-14 00:00:00 , DOI: 10.1021/acsomega.8b01378
Hairui Bai , Fujun Liu , Xiaojing Wang , Ping Wang , Chao Huang

The development of a clear chemical process to produce diverse value-added chemicals from low-cost raw materials is a particularly attractive concept and represents a considerable challenge in sustainable organic synthesis. Herein, two highly efficient and clear methods for the synthesis of quinolone derivatives based on a linear/branched domino protocol under sustainable conditions were established. The main advantages of these protocols are the simple experimental procedure, high bond-forming efficiency, inexpensive readily available starting materials, moderate to excellent yields with good functional group compatibility, and nonchromatographic purification, which render these methods particularly attractive for the sustainable preparation of biologically and medicinally interesting molecules. To demonstrate the practical utility of our protocol, existing pharmaceutical sarafloxacin was successfully synthesized. Furthermore, a postulated reaction pathway including condensation reaction/nucleophilic aromatic substitution/Friedel–Crafts reaction for these domino reactions is also discussed.

中文翻译:

通过线性/分支多米诺协议高效,可持续地合成功能化喹诺酮的三组分一罐法,喹诺酮类药物的氟沙星关键合成方法

开发一种从低成本原材料生产各种增值化学品的清晰化学工艺是一个特别有吸引力的概念,并且对可持续的有机合成提出了巨大的挑战。在此,建立了在线性和支链多米诺协议的基础上,在可持续条件下合成喹诺酮衍生物的两种高效,清晰的方法。这些规程的主要优点是简单的实验程序,高键形成效率,廉价的易得原料,中等至优异的收率以及良好的官能团相容性以及非色谱纯化,这些方法使得这些方法对于生物的可持续制备特别有吸引力。和医学上有趣的分子。为了证明我们的方案的实用性,成功地合成了现有的药物sarafloxacin。此外,还讨论了针对这些多米诺反应的假定反应路径,包括缩合反应/亲核芳族取代/ Friedel-Crafts反应。
更新日期:2018-09-14
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