Vargas Didier F, Larghi Enrique L, Kaufman Teodoro S
Instituto de Química Rosario (IQUIR, CONICET-UNR) and National University of Rosario (UNR), Suipacha 531, 2000 Rosario, Argentina.
ACS Omega. 2021 Jul 23;6(30):19356-19363. doi: 10.1021/acsomega.1c03082. eCollection 2021 Aug 3.
The broad-spectrum antiviral Remdesivir, a monophosphate nucleoside analogue prodrug (ProTide), was repurposed. In May 2020, it received emergency approval by the FDA, being the first drug approved to fight the new coronavirus (COVID-19) disease which targets the virus directly. The main synthetic strategies toward Remdesivir, and their relevant modifications, are presented and discussed, to provide a panoramic view of the state-of-the-art and the more important advances in this field. Recent progress, proposed improvements, and uses of novel technologies for the synthetic sequence are also detailed.
广谱抗病毒药物瑞德西韦,一种单磷酸核苷类似物前药(前药),被重新用于其他用途。2020年5月,它获得了美国食品药品监督管理局的紧急批准,成为首个被批准用于对抗新型冠状病毒(COVID-19)疾病的直接靶向该病毒的药物。本文介绍并讨论了瑞德西韦的主要合成策略及其相关修饰,以全景展示该领域的最新技术水平和更重要的进展。还详细介绍了合成序列的最新进展、提出的改进以及新技术的应用。