钯催化的γ-内酰胺与芳基氯（溴）的对映选择性芳基化反应构建季碳立体中心。
Palladium-Catalyzed Construction of Quaternary Stereocenters by Enantioselective Arylation of γ-Lactams with Aryl Chlorides and Bromides.
机构信息
Warren And Katharine Schlinger Laboratory for Chemistry and Chemical Engineering, Division of Chemistry and Chemical Engineering, California Institute of Technology, 1200 E. California Blvd. MC 101-20, Pasadena, CA, 91125, USA.
Dobo Hall, Department of Chemistry and Biochemistry, University of North Carolina, 601 S. College Rd., Wilmington, NC, 28403, USA.
出版信息
Angew Chem Int Ed Engl. 2019 Mar 22;58(13):4297-4301. doi: 10.1002/anie.201814475. Epub 2019 Feb 22.
Herein, we report the first Pd-catalyzed enantioselective arylation of α-substituted γ-lactams. Two sets of conditions were developed for this transformation, allowing for the use of either aryl chlorides or bromides as electrophiles. Utilizing a highly electron-rich dialkylphosphine ligand we have been able to construct α-quaternary centers in good yields (up to 91 % yield) and high enantioselectivities (up to 97 % ee).
在此，我们报告了首例 Pd 催化的 α-取代 γ-内酰胺的对映选择性芳基化反应。为了实现这一转变，我们开发了两种条件，允许使用芳基氯或溴作为亲电试剂。通过使用一种高度富电子的二烷基膦配体，我们能够以良好的收率（高达 91%的收率）和高对映选择性（高达 97%的 ee 值）构建α-季碳原子中心。
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