Densely functionalized chiral nitrogen-containing heterocycles are ubiquitous in bioactive synthetic compounds and natural products.Herein,we report a nickel(Ni)-catalyzed enantioselective desymmetrizing aza-Heck cycl...Densely functionalized chiral nitrogen-containing heterocycles are ubiquitous in bioactive synthetic compounds and natural products.Herein,we report a nickel(Ni)-catalyzed enantioselective desymmetrizing aza-Heck cyclization of oxime esters with a commercially available chiral pyridinebis(oxazoline)(pybox)ligand.This reaction proceeds under mild reaction conditions,tolerates various functional groups,and leads to chiral 2-substituted-3,7a-dihydro-3aH-indoles.展开更多
基金The authors are grateful for financial support from the Chinese Academy of Science(grant no.XDB20020000)the National Natural Science Foundation of China(no.21933004)+2 种基金the Shenzhen STIC(nos.JCYJ20170412150507046 and JCYJ20170412150343516)the Shenzhen San-Ming Project(no.SZSM201809085)fellowship from the International Postdoctoral Exchange Fellowship Program(no.2020014 to H.C.Shen).
文摘Densely functionalized chiral nitrogen-containing heterocycles are ubiquitous in bioactive synthetic compounds and natural products.Herein,we report a nickel(Ni)-catalyzed enantioselective desymmetrizing aza-Heck cyclization of oxime esters with a commercially available chiral pyridinebis(oxazoline)(pybox)ligand.This reaction proceeds under mild reaction conditions,tolerates various functional groups,and leads to chiral 2-substituted-3,7a-dihydro-3aH-indoles.