Regio‐ and Enantioselective Preparation of Chiral Allylic Sulfones Featuring Elusive Quaternary Stereocenters
作者:Aijie Cai、Arjan W. Kleij
DOI:10.1002/anie.201908318
日期:2019.10.14
We describe here the first general asymmetric synthesis of sterically encumbered α,α-disubstituted allylic sulfones via Pd-catalyzed allylic substitution. The design and application of a new and highly efficient phosphoramidite ligand (L10) proved to be crucial, and a wide variety of challenging allylic sulfones featuring quaternary stereocenters could be obtained in good yields and with good to excellent
我们在这里描述了通过Pd催化的烯丙基取代对位阻的α,α-二取代的烯丙基砜的首次一般不对称合成。事实证明,新型高效亚磷酰胺配体(L10)的设计和应用至关重要,可以在有吸引力的条件下以良好的收率和良好的区域和对映选择性水平获得各种各样具有四级立体中心的具有挑战性的烯丙基砜。工艺条件。开发的方法采用易于获得的化学原料,包括外消旋烯丙基前体和亚磺酸钠。通过倍半萜烯(-)-阿糖胞苷A的合成进一步证明了该方法的实用性。