Insights into Large-Scale Synthesis of Benfotiamine

IF 3.1 3区化学 Q2 CHEMISTRY, APPLIED Organic Process Research & Development Pub Date : 2024-10-14 DOI:10.1021/acs.oprd.4c00351

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

引用次数: 0

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.

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对大规模合成苯磷硫胺的见解

过去几年中，人们对合成苯磷硫胺的兴趣日益浓厚，这很可能是市场需求不断增长的直接结果。它的生物利用率比硫胺素（维生素 B1）高得多，因此更适合用于治疗目的，尤其是口服形式。我们在此报告我们在一个学术-私营研发项目中开展的研究，在该项目中，我们对小规模和大规模工艺的各个方面进行了研究。该工艺包括两个劳动密集型步骤，从盐酸硫胺素和关键中间体一磷酸硫胺素磷酸酯（TMP--一磷酸硫胺素的磷酸酯）开始。通过 XRD 粉末光谱、红外光谱和 RAMAN 分析，我们直接从合成中获得了市场上所需的晶体状苯磷硫胺。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Organic Process Research & Development 化学-应用化学

CiteScore

6.90

自引率

14.70%

发文量

251

审稿时长

2 months

期刊介绍： The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.