作者:Kevin J. Schwarz、Chao Yang、James W. B. Fyfe、Thomas N. Snaddon
DOI:10.1002/anie.201806742
日期:2018.9.10
esters is reported. This reaction proceeds via stereodefined C1‐ammonium enolate nucleophiles. Critical to its success was the identification of benzylic phosphate electrophiles, which were uniquely reactive. Alkylated products were obtained with very high levels of enantioselectivity, and this method has been applied toward the synthesis of the thrombin inhibitor DX‐9065a.
报道了无环酯的第一次不对称协作路易斯碱/钯催化的苄基烷基化。该反应通过立体定义的C1-烯醇铵盐亲核试剂进行。成功的关键是鉴定具有独特反应性的磷酸苄基亲电试剂。获得的烷基化产物具有很高的对映选择性,该方法已应用于凝血酶抑制剂DX‐9065a的合成。