Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad - 500037, India.
Org Biomol Chem. 2020 Dec 23;18(48):9737-9761. doi: 10.1039/d0ob01779e.
Microwave technology has emerged as a great tool for the efficient synthesis of organic compounds and it provides opportunities for chemists to achieve chemical transformations that tend to be challenging using classical approaches. Additionally, N-heterocycles are well-known for their medicinal/biological significance, along with their applications as excellent building blocks in chemical synthesis. The dominance of N-heterocycles in drug molecules and other pharmacological agents makes them attractive scaffolds, which encourages chemists to develop a wide range of strategies towards the greener synthesis and functionalization of these heterocycles. In this regard, we have collated and discussed literature relating to the microwave-assisted synthesis and the modification of non-(benzo)fused single-nitrogen-containing N-heterocycles from the past decade. The role of the microwave technique and its benefits over the conventional approach have also been emphasized in terms of overall reaction efficiency, reaction time, yield, reduced side-product generation, neat and clean reactions, chemo-/regio-/enantio-selectivity, and the use of mild reagents/reaction conditions to achieve the objectives of green and sustainable chemistry.
微波技术已成为高效合成有机化合物的重要工具,为化学家提供了实现化学转化的机会,这些转化往往使用经典方法具有挑战性。此外,杂环化合物因其药用/生物意义以及在化学合成中作为优秀构建块的应用而广为人知。杂环化合物在药物分子和其他药理制剂中的主导地位使它们成为有吸引力的支架,这促使化学家开发出广泛的策略,以实现这些杂环的更绿色合成和功能化。在这方面,我们收集并讨论了过去十年中有关微波辅助合成和非(苯并)稠合单氮含氮杂环修饰的文献。从总体反应效率、反应时间、产率、减少副产物生成、整洁干净的反应、化学选择性/区域选择性/对映选择性以及使用温和的试剂/反应条件来实现绿色和可持续化学的目标等方面强调了微波技术的作用及其相对于传统方法的优势。