申请人:DAIICHI SANKYO COMPANY, LIMITED
公开号:US10851111B2
公开(公告)日:2020-12-01
The present disclosure provides a method for efficiently producing and providing compounds having a spirooxindole skeleton, for example compounds having a spirooxindole skeleton and having antitumor activity that inhibit the interaction between Mdm2 protein and p53 protein, or intermediates thereof, using an asymmetric catalyst. Compounds having optically active tricyclic dispiroindole skeletons are obtained through catalytic asymmetric 1,3-dipolar cycloaddition reaction using ketimine as a reaction substrate and using a chiral ligand and a Lewis acid.
本公开提供了一种利用不对称催化剂高效生产和提供具有螺氧化吲哚骨架的化合物的方法,例如具有螺氧化吲哚骨架且具有抗肿瘤活性的抑制Mdm2蛋白和p53蛋白之间相互作用的化合物或其中间体。具有光学活性的三环二螺吲哚骨架的化合物是以酮亚胺为反应底物,使用手性配体和路易斯酸,通过催化不对称 1,3-二极环加成反应获得的。