期刊
TETRAHEDRON
卷 76, 期 37, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2020.131440
关键词
Enabling technologies; Evolution; Influenza; Tamiflu synthesis
资金
- Council for Scientific and Industrial Research-Department of Science and Technology, South Africa (CSIR-DST Grant)
- National Research Foundation (NRF SARChI Grant)
- Nelson Mandela University
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. (C) 2020 Elsevier Ltd. All rights reserved.
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