Synthesis of Dolutegravir Exploiting Continuous Flow Chemistry
Category
Published on CMKC
Abstract
An efficient continuous flow process for the synthesis of dolutegravir, an active pharmaceutical ingredient (API) for HIV treatment, was investigated. The synthetic procedure starts from a readily available benzyl-protected pyran via six chemical transformations using continuous flow reactors. The significant advantage of this flow process includes the reduction of the overall reaction time from 34.5 h in batch to 14.5 min. The overall yield of each reaction step improved dramatically upon flow optimization. Another key feature of this synthesis is telescoping multiple steps.
Journal
Journal of Organic Chemistry. Volume 88, 2023, 12024–12040
DOI
10.1021/acs.joc.3c01365
Type of publication
Peer-reviewed journal
Affiliations
- Nelson Mandela University
Article Classification
Research Article
Classification Areas
- API