Preparation of goniothalamin under flow reaction conditions

Abstract

Flow chemistry is the process of performing chemical reactions in a tube or pipe. Reactive components are pumped together at a mixing junction and flowed down a temperature and pressure controlled tube. The major advantages of flow chemistry are faster reactions, cleaner products, safer reactions, quick reaction optimization, easy scale-up, and the integration of typically separate processes (such as synthesis, work-up and analysis). This flow technology has been applied quite successfully in multi-step synthesis of biologically active compounds. In an ongoing program to identify new candidates for cancer treatment, goniothalamin was recognized as a good lead compound with significant cytotoxic and antiproliferative activities against a variety of tumor cell lines. Due to our continuous effort to evaluate new goniothalamin analogues and the high potential of the flow chemistry to the synthesis of natural products and biologically active compounds, in this project we intend to explore this technology for large-scale preparation of goniothalamin and more potent derivatives. The process developed could accelerate the discovery of new anticancer agents, since the biological assays, typically performed in vivo, requires a large amount of material. (AU)