The Development of Synthetic Routes Leading to Pharmaceuticals and the Key Intermediates Using Hydroxynitrile Lyase

In this investigation, we developed several novel synthetic routes using hydroxynitrile lyase (HNL) from <i>Parafontaria laminata</i> (PlamHNL) to synthesize active pharmaceutical ingredients, specifically Cenobamate (Xcopri), Clopidogrel (Plavix), and Mirabegron (Myrbetriq). Our methods demonstrate higher enantioselectivity, improved regioselectivity, and better yields. Notably, both Xcopri and Clopidogrel are produced from a common intermediate, (<i>R</i>)-methyl-2-chloro mandelate.

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Publication Details

Journal
The Journal of Organic Chemistry
Published
2025-05-22
DOI
https://doi.org/10.1021/acs.joc.5c00427
Citations
2
Primary Topic
Analytical Chemistry and Chromatography
Type
article
Field-Weighted Citation Impact
1.51

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article

The Development of Synthetic Routes Leading to Pharmaceuticals and the Key Intermediates Using Hydroxynitrile Lyase

Genji Iwasaki, J.N. Chakraborty, Yasuhisa Asano
2 citations
The Journal of Organic Chemistry
Analytical Chemistry and Chromatography
1.51
article

The Development of Synthetic Routes Leading to Pharmaceuticals and the Key Intermediates Using Hydroxynitrile Lyase

Genji Iwasaki, J.N. Chakraborty, Yasuhisa Asano
article en
2 citations

Abstract

In this investigation, we developed several novel synthetic routes using hydroxynitrile lyase (HNL) from <i>Parafontaria laminata</i> (PlamHNL) to synthesize active pharmaceutical ingredients, specifically Cenobamate (Xcopri), Clopidogrel (Plavix), and Mirabegron (Myrbetriq). Our methods demonstrate higher enantioselectivity, improved regioselectivity, and better yields. Notably, both Xcopri and Clopidogrel are produced from a common intermediate, (<i>R</i>)-methyl-2-chloro mandelate.

The Journal of Organic ChemistryVol. 90(22)
Toyama Prefectural University (JP)
Japan Society for the Promotion of Science
Openalex Percentile: Top 19%
Analytical Chemistry and Chromatography
1.51
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