Department of Pharmaceutical Chemistry, Faculty of Pharmacy, National and Kapodistrian University of Athens, 15771, Athens, Greece.
ChemMedChem. 2020 Mar 5;15(5):392-403. doi: 10.1002/cmdc.201900682. Epub 2020 Feb 12.
Morpholine is a frequently used heterocycle in medicinal chemistry and a privileged structural component of bioactive molecules. This is mainly due to its contribution to a plethora of biological activities as well as to an improved pharmacokinetic profile of such bioactive molecules. The synthesis of morpholines is a subject of much study due to their biological and pharmacological importance, with the last such review being published in 2013. Here, an overview of the main approaches toward morpholine synthesis or functionalization is presented, emphasizing on novel work which has not been reviewed so far. This review is an update on synthetic strategies leading to easily accessible libraries of bioactives which are of interest for drug discovery projects.
吗啡啉是药物化学中常用的杂环，也是生物活性分子的特权结构组成部分。这主要是由于其对多种生物活性的贡献，以及对这些生物活性分子的药代动力学特性的改善。由于吗啡啉的生物学和药理学重要性，它们的合成一直是一个研究热点，最后一次综述发表于 2013 年。本文概述了吗啡啉合成或功能化的主要方法，重点介绍了迄今尚未综述的新工作。本文综述了合成策略，这些策略可以得到易于获得的生物活性文库，这些文库对药物发现项目有意义。
