Department of Chemistry and Institute of Basic Science, Sungkyunkwan University, Suwon, 16419, Korea.
Angew Chem Int Ed Engl. 2021 Feb 23;60(9):4614-4618. doi: 10.1002/anie.202014425. Epub 2021 Jan 12.
We report the diastereo- and enantioselective conjugate addition of chiral secondary borylalkyl copper species derived from borylalkenes in situ to α,β-unsaturated diesters. In the presence of a chiral bisphosphine-ligated CuH catalyst, the conjugate addition provides a direct access to enantioenriched alkylboron compounds containing two contiguous carbon stereogenic centers in good yield with high diastereo- and enantioselectivity (up to >98:2 dr, >99:1 er) by assembling readily available starting alkenyl reagents in a single operation without using preformed organometallic reagents or chiral auxiliaries. The resulting products were used in various organic transformations. The utility of the synthetic approach was highlighted by the synthesis of (-)-phaseolinic acid.
我们报告了手性仲硼酸酯铜物种的非对映选择性和对映选择性共轭加成,该物种是由原位生成的硼烯与α,β-不饱和二酯反应得到的。在手性双膦配体 CuH 催化剂的存在下,通过单一操作组装易得的烯基试剂,无需使用预形成的有机金属试剂或手性助剂,该共轭加成反应以高收率和高非对映选择性和对映选择性(高达 >98:2 dr,>99:1 er)提供了直接获得含有两个连续碳手性中心的手性烷基硼化合物的方法。所得产物可用于各种有机转化。该合成方法的实用性通过 (-)-phaseolinic 酸的合成为例得到了强调。