Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.
Molecules. 2020 Jul 10;25(14):3161. doi: 10.3390/molecules25143161.
We developed an efficient microwave-assisted three-step synthesis of zolpidem and its fluorinated analogues -. 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 , 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 -, as well as zolpidem tartrate salt with suitable fine-particle size for further biological experimentation.
我们开发了一种高效的微波辅助三步合成唑吡坦及其氟化类似物的方法。该方法依赖于使用易于获得且廉价的起始原料。与传统加热系统相比，我们的方案在产物的产率和纯度方面表现出优异的性能。值得注意的是，与油浴加热系统相比，反应完成所需的总时间明显更短。最后，我们对酒石酸唑吡坦盐的制备进行了详细的研究，并使用偏光显微镜评估了其颗粒尺寸。我们的目标是选择合适的方法来获得可接受的粒径，因为固体粒径直接影响在生物流体中的溶解度和进一步的生物利用度。我们相信，所公开的程序将有助于生产唑吡坦及其氟化衍生物以及酒石酸唑吡坦盐的实验室规模数量，以及具有适合进一步生物学实验的细颗粒尺寸的酒石酸唑吡坦盐。
