Atropisomerism as inspiration for new chemistry

Atropisomerism as inspiration for new chemistry
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DOI:
10.24820/ark.5550190.p011.382
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发表时间:
2021-01-01
期刊:
影响因子:
0.9
通讯作者:
Gustafson, Jeffrey L.
Gustafson, Jeffrey L.
中科院分区:
化学4区
文献类型:
--
作者:
Cardenas, Mariel M.;Nguyen, Ashley D.;Gustafson, Jeffrey L.

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异构性是一种手性,在现代药物开发中无处不在,但常常被忽视。在这篇文章中,我们讨论了在药物化学中利用阿托品异构化作为设计原则的研究,以及这项工作如何导致了几个看似不同的项目,这些项目是由于与获得药物相关的阿托品相关的合成挑战而开始的。
Atropisomerism is a type of chirality that is ubiquitous but often overlooked in modern drug discovery. In this Account we discuss studies on leveraging atropisomerism as a design principle in medicinal chemistry, and how this work led to several seemingly disparate projects that began due to synthetic challenges associated with accessing pharmaceutically relevant atropisomers.[GRAPHICS].