Abstract
We developed an efficient microwave-assisted three-step synthesis of zolpidem and its fluorinated analogues 1–3. The procedure relays on the utilization of easily accessible and inexpensive starting materials. Our protocol shows superior performance in terms of yield and purity of products, compared to conventional heating systems. Notably, the total time needed for reaction accomplishment is significantly lower comparing to oil bath heating systems. Finally, we have performed a detailed study on the preparation of zolpidem tartrate salt I, and we assessed its particle-sizes using a polarizing microscope. Our goal was to select the appropriate method that generates the acceptable particle-size, since the solid-size directly influences solubility in biological fluids and further bioavailability. We believe that the disclosed procedure will help to produce a lab-scale quantity of zolpidem and its fluorinated derivatives 1–3, as well as zolpidem tartrate salt I, with suitable fine-particle size for further biological experimentation.
Highlights
Zolpidem 1 is one of the most widely prescribed hypnotic medications in the United States, with an annual prescription rate of nearly 39 million [1,2]
We suspect that the improved performance in toluene mainly depended on the formation of ‘hot spots’, produced by increased microwave absorption at the surface of the insoluble formation of ‘hot spots’, produced by increased microwave absorption at the surface of the insoluble
We have disclosed a practical procedure for delivering lab-scale quantities of zolpidem 1 and its fluorinated 2–3 analogues, incorporating microware supported chemistry
Summary
Zolpidem 1 is one of the most widely prescribed hypnotic medications in the United States, with an annual prescription rate of nearly 39 million [1,2]. Zolpidem has featured in several curious case reports that documented the reversal of brain stroke symptoms [6], improvement of motor dysfunction in Parkinson’s disease patients [7] or the effective reduction of chronic pain [8]. All these unique features are attributed to the enhanced synaptic GABA-ergic currents in specific brain regions.
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