Johannes Burkhard

We report the process development and a streamlined synthesis of the highly substituted quinazoline core present in GDC-6036, an exceedingly selective and potent inhibitor of the G12C mutant isoform of KRAS…

We report the process development for the endgame synthesis of GDC-6036, a highly selective and potent inhibitor of the G12C mutant isoform of KRAS, for both early and late-stage clinical deliveries…

An enabling synthesis of tricyclo[6.2.0.03,6]deca-1,3(6),7-trien-2-amine was developed starting from _p_-phenylenediacetic acid, which was first converted in four steps to 1,4-dibromo-2,5-bis(2-bromoethyl)benzene and then subjected to Parham cyclization conditions…