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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.

DOI:10.1016/j.tetlet.2008.11.121
PMID:20160840
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2631556/
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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Antimicrob Agents Chemother. 2008 Nov;52(11):3915-21. doi: 10.1128/AAC.00330-08. Epub 2008 Sep 2.
2
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Syntheses of quinazoline-2,4-dione alkaloids and analogues from Mexican Zanthoxylum species.从墨西哥花椒属植物中合成喹唑啉-2,4-二酮生物碱及其类似物。
Molecules. 2004 Jun 30;9(7):609-16. doi: 10.3390/90700609.
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