Sagandira Cloudius R, Mathe Francis M, Guyo Upenyu, Watts Paul
Nelson Mandela University, University Way, Port Elizabeth, 6031, South Africa.
Midlands State University, Senga Road, Gweru, Zimbabwe.
Tetrahedron. 2020 Sep 11;76(37):131440. doi: 10.1016/j.tet.2020.131440. Epub 2020 Jul 26.
Influenza is a serious respiratory disease responsible for significant morbidity and mortality due to both annual epidemics and pandemics; its treatment involves the use of neuraminidase inhibitors. (-)-Oseltamivir phosphate (Tamiflu) approved in 1999, is one of the most potent oral anti-influenza neuraminidase inhibitors. Consequently, more than 70 Tamiflu synthetic procedures have been developed to date. Herein, we highlight the evolution of Tamiflu synthesis since its discovery over 20 years ago in the quest for a truly efficient, safe, cost-effective and environmentally benign synthetic procedure. We have selected a few representative routes to give a clear account of the past, present and the future with the advent of enabling technologies.
流感是一种严重的呼吸道疾病，每年的流行和大流行都会导致大量发病和死亡；其治疗涉及使用神经氨酸酶抑制剂。1999年获批的（-）-磷酸奥司他韦（达菲）是最有效的口服抗流感神经氨酸酶抑制剂之一。因此，迄今为止已开发出70多种达菲的合成方法。在此，我们着重介绍自达菲20多年前被发现以来其合成方法的演变，以寻求一种真正高效、安全、经济且环境友好的合成方法。我们选择了一些具有代表性的路线，以便随着使能技术的出现清晰地阐述其过去、现在和未来。
