Chong Han

This presentation will highlight process chemistry efforts at Genentech that led to an efficient synthesis of PI3K inhibitor GDC-0077, featuring two consecutive Cu-catalyzed C–N coupling reactions…

Highly diastereoselective syntheses of tetrasubstituted alkenes via nickel-catalyzed Suzuki-Miyaura cross-couplings of enol tosylates and arylboronic esters were developed…

We report our process chemistry efforts in developing an efficient synthesis of a KRAS G12C inhibitor. The target compound features a heavily substituted quinoline core bearing rotationally locked biaryl group…

We report an efficient synthesis of 3-functionalized 4-quinolones, a class of privileged pharmacophores found in numerous biologically and pharmaceutically active compounds…

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…

We present our process chemistry efforts in developing an efficient synthesis of a highly substituted aryl boronic acid building block for a KRAS G12C brain-penetrant inhibitor…