Process Intensification of a Napabucasin Manufacturing Method Utilizing Microflow Chemistry.

Microflow chemistry is one of the newest and most efficient technologies used today for the safe and effective production of medicines. In this paper, we show the use of this technology in the development of a manufacturing method for napabucasin, which has potential in the treatment of colorectal and pancreatic cancers. In conventional "batch-type" reactor systems, the generation of side products can be controlled with traditional techniques such as reagent reverse-addition and temperature control. However, there is a limitation to which the yield and purity can be improved by these methods, as both are constrained by the efficiency of heat/mass transfer. Applying microflow chemistry technology alters the parameters of the constraint through the use of precise mixing in a microchannel, which offers increased possibility for improving yields and process intensification of the napabucasin process. Reported herein is a proof-of-concept study for the scale-up production of napabucasin using microflow chemistry techniques for manufacturing at the kilogram scale.