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，由于每年的流行病和大流行，导致很高的发病率和死亡率；其治疗涉及使用神经氨酸酶抑制剂。 (−)-磷酸奥司他韦（达菲）于 1999 年获得批准，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 多种达菲合成程序。在此，我们重点介绍自 20 多年前发现达菲以来合成的演变，以寻求真正高效、安全、经济高效且环境友好的合成程序。我们选择了几条具有代表性的路线，以清晰地讲述使能技术的过去、现在和未来。