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.

中文翻译：

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苯磷硫胺大规模合成的见解


在过去几年中，人们对苯磷硫胺的合成越来越感兴趣，这很可能是市场需求不断增长的直接结果。它的生物利用度比硫胺素（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学术私人研发项目中的研究，在这个项目中，我们调查了小规模和大规模过程的所有方面。该程序涉及两个劳动密集型步骤，从盐酸硫胺三烯和关键的中间体磷酸硫胺素（TMP─一磷酸硫胺素的磷酸酯）开始。我们直接从合成中以市场上所需的结晶形式获得了苯磷硫胺的结晶形式，XRD 粉末光谱、红外和拉曼光谱证实了这一点。