KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
申请人:AMGEN INC.
公开号:US20180177767A1
公开(公告)日:2018-06-28
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
α-Methylene carbonyl compounds are regioselectively prepared by the reaction of α-nitroketones or α-nitroesters with 37% formaldehyde in the presence of a catalytic amount of weak bases followed by acetylation, denitration with Bu3SnH, and elimination of acetic acid.