2-氨基-6-氯-4-环丙基-7-氟-5-甲氧基-吡啶并[1,2-c]嘧啶-1,3-二酮核心环系的高效合成
Efficient Synthesis of the 2-amino-6-chloro-4-cyclopropyl-7-fluoro-5-methoxy-pyrido[1,2-c]pyrimidine-1,3-dione core ring system.
作者信息
Rosen Jonathan D, German Nadezhda, Kerns Robert J
机构信息
Division of Medicinal & Natural Products Chemistry, University of Iowa, Iowa City, Iowa 52242, USA.
出版信息
Tetrahedron Lett. 2009 Feb 18;50(7):785-789. doi: 10.1016/j.tetlet.2008.11.121.
Abstract
An optimized total synthesis of the 2-amino-6-chloro-4-cyclopropyl-7-fluoro-5-methoxy-pyrido[1,2-c]pyrimidine-1,3-dione core structure of a new fluoroquinolone-like class of antibacterial agents is described. This synthesis is highlighted by a nearly quantitative ring-closing reaction to form the pyrido[1,2-c]pyrimidine core. This bicyclic ring system serves as a scaffold for a family of biologically active compounds.
摘要
描述了一种新型氟喹诺酮类抗菌剂的2-氨基-6-氯-4-环丙基-7-氟-5-甲氧基-吡啶并[1,2-c]嘧啶-1,3-二酮核心结构的优化全合成方法。该合成方法的亮点是通过近乎定量的闭环反应形成吡啶并[1,2-c]嘧啶核心。这种双环系统作为一系列生物活性化合物的骨架。
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