(KRAZATI TM ) -leading to a significant increase in antitumor activity in comparison with their respective activity as a single agent. 3 The route to MRTX0902 developed by our drug discovery colleagues (Scheme 1) was used to deliver several kilograms of crucial intermediates while also providing sufficient amount of active pharmaceutical ingredient (API) to support early stage studies. However, while this route was effective for initial development, several improvements were necessary in order to prepare multi-kilogram amount of API for GLP toxicology and FIH studies.