An improved process for the preparation of tenofovir disoproxil fumarate
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Date
Authors
Riley, Darren Lyall
Walwyn, David Richard
Edlin, Chris D.
Journal Title
Journal ISSN
Volume Title
Publisher
American Chemical Society
Abstract
The current three-step manufacturing route for the preparation of tenofovir disoproxil fumarate (1) was assessed and optimized leading to a higher yielding, simpler and greener process. Key improvements in the process route include the refinement of the second stage through the replacement of the problematic magnesium tert-butoxide (MTB) with a 1:1 ratio of a Grignard reagent and tert-butanol. The development of a virtually solvent-free approach and the establishment of a work-up and purification protocol which allows the isolation of a pure diethyl phosphonate ester (8).
Description
Keywords
Tenofovir, Tenofovir disoproxil fumarate, Manufacturing route, Process route
Sustainable Development Goals
Citation
Riley, DL, Walwyn, DR & Edlin, CD 2016, 'An improved process for the preparation of tenofovir disoproxil fumarate', Organic Process Research and Development, vol. 20, no. 4, pp. 742-750.