Braga Felipe C, Ramos Tiago O, Brocksom Timothy J, de Oliveira Kleber T
Department of Chemistry, Federal University of São Carlos, São Carlos, São Paulo 13565-905, Brazil.
Org Lett. 2022 Nov 18;24(45):8331-8336. doi: 10.1021/acs.orglett.2c03338. Epub 2022 Nov 8.
An advantageous and original synthesis of fentanyl is described. This new approach includes two efficient continuous flow reductive aminations achieved via photoredox catalysis and a final batch acylation. A telescoped protocol for the two photocatalyzed steps is also presented, and overall, this protocol provides improved sustainability, significant efficiency, reduced temperatures and reaction times, and is functional for scaling up this relevant active pharmaceutical ingredient (API).
描述了一种芬太尼的有利且新颖的合成方法。这种新方法包括通过光氧化还原催化实现的两个高效连续流还原胺化反应以及最后的间歇酰化反应。还介绍了两个光催化步骤的串联方案,总体而言,该方案提高了可持续性、显著提高了效率、降低了温度和反应时间,并且适用于扩大这种相关活性药物成分(API)的规模。