点击转化腈（RCN）为噁唑基砜基氟弹头。
Clickable Transformation of Nitriles (RCN) to Oxazolyl Sulfonyl Fluoride Warheads.
机构信息
State Key Laboratory of Silicate Materials for Architectures; and School of Chemistry, Chemical Engineering and Life Sciences, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, People's Republic of China.
School of Life Science, Wuchang University of Technology, Wuhan, 430223, People's Republic of China.
出版信息
Org Lett. 2020 Nov 20;22(22):8904-8909. doi: 10.1021/acs.orglett.0c03298. Epub 2020 Nov 9.
The protocol for simple, efficient, and mild synthesis of oxazolyl sulfonyl fluorides was developed through Rh(OAc)-catalyzed annulation of methyl-2-diazo-2-(fluorosulfonyl)acetate (MDF) or its ethyl ester derivative with nitriles. This practical method provides a general and direct route to a unique class of highly functionalized oxazolyl-decorated sulfonyl fluoride warheads with great potential in medicinal chemistry, chemical biology, and drug discovery.
通过 Rh(OAc)催化的甲酯-2-重氮-2-(氟磺酰基)乙酸酯（MDF）或其乙酯衍生物与腈的环加成反应，开发了一种简单、高效、温和的合成噁唑基磺酰氟的方法。这种实用的方法为具有潜在药用化学、化学生物学和药物发现价值的一类独特的高度官能化的噁唑基取代的磺酰氟弹头提供了一种通用而直接的途径。
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