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 (TMPthe 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.