An Efficient Synthesis of Tenofovir (PMPA): A Key
Intermediate Leading to Tenofovir-Based HIV Medicines
Posted on 2020-07-10 - 23:43
Herein, we report further improvements
to the synthesis of tenofovir 1, the precursor to tenofovir
disoproxil fumarate (TDF) and
tenofovir alafenamide fumarate (TAF). Starting from acyclic precursor
diaminomalononitrile 12, a four-step protocol to tenofovir 1 will allow for vertical integration for more manufacturers.
The key transformation is a convergent one-step procedure from 6 as compared to the current commercial process, with an improved
yield from 59% (two steps) to 70%. Further improvements include eliminating
the need for problematic magnesium tert-butoxide
(MTB) and significant solvent reduction by avoiding an intermediate
workup. With the costs of HIV/AIDS treatments remaining a barrier
for those most in need, lowering the raw material/processing costs
and increasing the security of supply can increase patient access.
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Derstine, Brenden
P.; Tomlin, John W.; Peck, Cheryl L.; Dietz, Jule-Phillip; Herrera, Brenden T.; Cardoso, Flavio S. P.; et al. (2020). An Efficient Synthesis of Tenofovir (PMPA): A Key
Intermediate Leading to Tenofovir-Based HIV Medicines. ACS Publications. Collection. https://doi.org/10.1021/acs.oprd.0c00078