Synthesis of Fused Pyrimidinone and Quinolone Derivatives in an Automated High-Temperature and High-Pressure Flow Reactor
作者:Jennifer Tsoung、Andrew R. Bogdan、Stanislaw Kantor、Ying Wang、Manwika Charaschanya、Stevan W. Djuric
DOI:10.1021/acs.joc.6b02520
日期:2017.1.20
pyrimidinone and quinolone derivatives that are of potential interest to pharmaceutical research were synthesized within minutes in up to 96% yield in an automated Phoenix high-temperature and high-pressure continuous flow reactor. Heterocyclic scaffolds that are either hard to synthesize or require multisteps are readily accessible using a common set of reaction conditions. The use of low-boiling solvents
在自动化的Phoenix高温高压连续流反应器中,数分钟之内即可合成出对药物研究潜在感兴趣的熔融嘧啶酮和喹诺酮衍生物,收率高达96%。难于合成或需要多步操作的杂环支架可使用一组常见的反应条件轻松获得。低沸点溶剂的使用以及这些反应的高转化率使得易于后处理和分离。本文报道的方法高度适合于快速和有效的杂环合成以及化合物的放大。