Insights into Large-Scale Synthesis of Benfotiamine

There has been increased interest in the synthesis of benfotiamine during the past few years, most likely as a direct consequence of growing market demand. It has much higher bioavailability than thiamine (vitamin B1) and therefore is more suitable for therapeutic purposes, especially in oral form. We report herein our research in an academic-private R&D project in which we investigate all aspects of the process on small and large scales. The procedure involves two labor-intensive steps, starting from thiami3ne chloride hydrochloride with the key intermediate thiamine monophosphate phosphate (TMP─the phosphate ester of thiamine monophosphate). We obtained the crystalline form of benfotiamine directly from the synthesis in the crystalline form required on the market, as proven by XRD powder spectroscopy, IR, and RAMAN.

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Publication Details

Journal
Organic Process Research & Development
Published
2024-10-14
DOI
https://doi.org/10.1021/acs.oprd.4c00351
Citations
2
Primary Topic
N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
Type
article
Field-Weighted Citation Impact
0.50

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article

Insights into Large-Scale Synthesis of Benfotiamine

Nicoleta Sandu, Oana-Cristina Maximov, Codruța C. Popescu, Maxim Maximov et al.
2 citations
Organic Process Research & Development
N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
0.50
article

Insights into Large-Scale Synthesis of Benfotiamine

Nicoleta Sandu, Oana-Cristina Maximov, Codruța C. Popescu, Maxim Maximov, Anca G. Mirea, Mihaela Florea, Daniel P. Funeriu, Anamaria Hanganu, Mihaela Matache, Cristian Gârbea
article en
2 citations

Abstract

There has been increased interest in the synthesis of benfotiamine during the past few years, most likely as a direct consequence of growing market demand. It has much higher bioavailability than thiamine (vitamin B1) and therefore is more suitable for therapeutic purposes, especially in oral form. We report herein our research in an academic-private R&D project in which we investigate all aspects of the process on small and large scales. The procedure involves two labor-intensive steps, starting from thiami3ne chloride hydrochloride with the key intermediate thiamine monophosphate phosphate (TMP─the phosphate ester of thiamine monophosphate). We obtained the crystalline form of benfotiamine directly from the synthesis in the crystalline form required on the market, as proven by XRD powder spectroscopy, IR, and RAMAN.

Organic Process Research & DevelopmentVol. 28(11)
University of Bucharest (RO), National Institute of Materials Physics (RO), Romanian Academy (RO), Universitatea Națională de Știință și Tehnologie Politehnica București (RO)
Unitatea Executiva pentru Finantarea Invatamantului Superior, a Cercetarii, Dezvoltarii si Inovarii, Universitatea din București
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Openalex Percentile: Top 39%
N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
0.50
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