化学
分子内力
立体中心
赫克反应
对映选择合成
催化作用
磷酰胺
烯烃
邻接
吲哚试验
组合化学
药物化学
有机化学
钯
DNA
生物化学
寡核苷酸
作者
Wang Bi,Jing Gao,Shuai Sun,Zhenlu Shen,Yun‐Fang Yang,Ren‐Xiao Liang,Yi‐Xia Jia
标识
DOI:10.1021/acs.orglett.4c00775
摘要
An enantioselective Pd-catalyzed intramolecular dearomative reductive Heck reaction of N-(o-bromoaryl) indole-3-carboxamide is developed. By employing Pd(dba)2/SPINOL-based phosphoramidite as the chiral catalyst and HCO2Na as the hydride source, a series of enantioenriched spiro indolines bearing vicinal stereocenters were afforded in moderate to good yields with excellent enantioselectivities. The reductive Heck reaction of formal tetrasubstituted alkene bearing β-hydrogens is therefore realized by inhibiting β-H elimination.
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