Discovery Chemistry and Technologies, AbbVie, Inc. , 1 North Waukegan Road, North Chicago, Illinois 60064, United States.
Department of Medicinal Chemistry, University of Kansas , Lawrence, Kansas 66047, United States.
J Org Chem. 2017 Jan 20;82(2):1073-1084. doi: 10.1021/acs.joc.6b02520. Epub 2017 Jan 10.
Fused 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 along with the high conversions of these reactions allowed for facile workup and isolation. The methods reported herein are highly amenable for fast and efficient heterocycle synthesis as well as compound scale-ups.
在 Phoenix 高温高压连续流反应器中，几分钟内即可完成潜在有药用价值的融合嘧啶酮和喹诺酮衍生物的合成，最高产率可达 96%。使用一套通用的反应条件，即可轻易获得那些难以合成或需要多步反应的杂环支架。这些反应采用低沸点溶剂，并具有较高的转化率，这使得后处理和分离变得简单。本文所报道的方法非常适合快速有效地合成杂环化合物，也适合进行化合物的规模化生产。
