<br/>Islatravir is an investigational nucleoside reverse transcriptase translocation inhibitor (NRTTI) currently being evaluated in clinical trials for the treatment of HIV infection. The manufacturing route involves a novel enzymatic cascade between an elaborated ribose fragment and 2-fluoroadenine (2-FA). 2-FA is a significant contributor to the API cost and its commercial availability is limited. A green manufacturing process has been developed to deliver 2-FA from commodity chemicals, involves an efficient & mild difluorination reaction using readily available potassium fluoride at ambient temperature, a highly selective direct amination and a simple deprotection in water. Final in-situ release of 2-FA in water with a catalytic amount of acid provides the ideal particle size for the enzymatic cascade end game to deliver final API, eliminating isolation and pin-milling of 2-FA to maximize operation simplicity.

Innovative process development to access 2-fluoroadenine for islatravir

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.