Meher Sushanta Kumar, Velpuri Venkateswara Rao, Naikwade Shyamali Rajendra, Peruncheralathan Saravanan, Venkatasubbaiah Krishnan
School of Chemical Sciences, National Institute of Science Education and Research (NISER), Bhubaneswar, an OCC of Homi Bhabha National Institute, Bhubaneswar-752050, Odisha, India.
J Org Chem. 2024 Sep 6;89(17):12785-12789. doi: 10.1021/acs.joc.4c01222. Epub 2024 Aug 20.
We report a simple synthetic method for obtaining 3-hydroxy-4,5-disubstituted isothiazoles utilizing dithioester and aryl acetonitrile. The isothiazoles obtained in this method involve the formation of new C-C, C-O, and N-S bonds in one step using a simple base such as KOH under aerial conditions. The 3-hydroxy-4,5-disubstituted isothiazole was successfully employed for further functionalization. The strategy provides high selectivity for the synthesis of isothiazoles, which may have applications in pharmaceuticals, organic materials, and agrochemicals in both academic and industrial settings.
我们报道了一种利用二硫酯和芳基乙腈制备3-羟基-4,5-二取代异噻唑的简单合成方法。通过该方法得到的异噻唑涉及在空气中使用诸如氢氧化钾之类的简单碱一步形成新的C-C、C-O和N-S键。3-羟基-4,5-二取代异噻唑已成功用于进一步官能化。该策略为异噻唑的合成提供了高选择性，在学术和工业领域的药物、有机材料及农用化学品方面可能具有应用价值。
