Process Chemistry / Route Selection are important activities in the path of a drug from mind to market. The medicinal chemistry routes for synthesis, although amenable to analogue design, are usually low yielding and are fraught with a plethora of intractable problems such as such as commercially unavailable reagents and intermediates, capricious and cryogenic reactions that preclude efficient scale up, tedious chromatography unfavorable atom economy and problems in waste disposal and management. Considerable research efforts must be expended in developing novel, cost efficacious and scalable processes, and seamlessly transferring these technologies to manufacturing operations. These principles will be demonstrated by our award-winning process development efforts that have resulted in amelioration of many of these problems and removal of significant bottlenecks in the progress of a drug from conception to commercialization. Our work also led to the discovery of NCEs exemplifying our concepts of “Process Chemistry Driven Medicinal Chemistry”