An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine

[Image: see text] An 11-step, 8-pot synthesis of the antimalarial drug tafenoquine succinate was achieved in 42% overall yield using commercially available starting materials. Compared to the previous manufacturing processes that utilize environmentally egregious organic solvents and toxic reagents,...

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Autores principales: Kavthe, Rahul D., Kincaid, Joseph R. A., Lipshutz, Bruce H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9768812/
https://www.ncbi.nlm.nih.gov/pubmed/36569493
http://dx.doi.org/10.1021/acssuschemeng.2c05628
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author Kavthe, Rahul D.
Kincaid, Joseph R. A.
Lipshutz, Bruce H.
author_facet Kavthe, Rahul D.
Kincaid, Joseph R. A.
Lipshutz, Bruce H.
author_sort Kavthe, Rahul D.
collection PubMed
description [Image: see text] An 11-step, 8-pot synthesis of the antimalarial drug tafenoquine succinate was achieved in 42% overall yield using commercially available starting materials. Compared to the previous manufacturing processes that utilize environmentally egregious organic solvents and toxic reagents, the current route features a far greener (as measured by Sheldon’s E Factors) and likely more economically attractive sequence, potentially expanding the availability of this important drug worldwide.
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spelling pubmed-97688122022-12-22 An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine Kavthe, Rahul D. Kincaid, Joseph R. A. Lipshutz, Bruce H. ACS Sustain Chem Eng [Image: see text] An 11-step, 8-pot synthesis of the antimalarial drug tafenoquine succinate was achieved in 42% overall yield using commercially available starting materials. Compared to the previous manufacturing processes that utilize environmentally egregious organic solvents and toxic reagents, the current route features a far greener (as measured by Sheldon’s E Factors) and likely more economically attractive sequence, potentially expanding the availability of this important drug worldwide. American Chemical Society 2022-12-07 2022-12-19 /pmc/articles/PMC9768812/ /pubmed/36569493 http://dx.doi.org/10.1021/acssuschemeng.2c05628 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by/4.0/Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Kavthe, Rahul D.
Kincaid, Joseph R. A.
Lipshutz, Bruce H.
An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine
title An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine
title_full An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine
title_fullStr An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine
title_full_unstemmed An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine
title_short An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine
title_sort efficient and sustainable synthesis of the antimalarial drug tafenoquine
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9768812/
https://www.ncbi.nlm.nih.gov/pubmed/36569493
http://dx.doi.org/10.1021/acssuschemeng.2c05628
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