公开(公告)号：US20250101006A1

公开(公告)日：2025-03-27

申请号：US18834099

申请日：2023-01-30

Applicant: NOVARTIS AG

Inventor： Markus BAENZIGER ,  Fabrice GALLOU ,  Fengfeng GUO ,  Rudolf HÄNGGI ,  Enjian HAN ,  Guido JORDINE ,  Jialiang LI ,  Weipeng LIU ,  Bukeyan MIAO ,  Shaofeng RONG ,  Ernesto SANTANDREA ,  Paul Bernd SCHIRNER ,  Xiaodong SHEN ,  Can WANG ,  Hao ZHANG

IPC: C07D403/14 ,  B01J31/22 ,  B01J31/24

Abstract: The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.