Route Development toward a Pyrazine Building Block to Enable Early Scale-Up Campaigns

We required rapid access to hundreds of grams of a key building block to support early scale-up campaigns during one of our Oncology programs. Accordingly, we report herein the exploration of two synthetic approaches to this compound by our Discovery Process team. This work culminated in the development and optimization of a phase-appropriate synthetic route that was successfully utilized by one of our contract development and manufacturing organizations (CDMOs) to quickly deliver 300 g of intermediate 1•TsOH.