ETH Zürich, HCI H335, 8093 Zürich, Switzerland.
Angew Chem Int Ed Engl. 2013 Jul 15;52(29):7532-5. doi: 10.1002/anie.201302731. Epub 2013 May 27.
No leaving group needed: With an Ir(P,olefin) complex as catalyst, the direct enantioselective allylic alkynylation of secondary allylic alcohols with potassium alkynyltrifluoroborates as alkynylating reagents has been achieved. High levels of enantioselectivity and high yields were achieved with this operationally easy and robust protocol, the use of which was demonstrated in the synthesis of GPR40 receptor agonist AMG 837. cod = 1,5-cyclooctadiene.
以 Ir(P,olefin) 配合物为催化剂,通过钾炔基三氟硼酸盐作为炔基化试剂,实现了二级烯丙醇与炔基三氟硼酸盐的直接对映选择性烯丙基炔基化反应。该操作简单、稳定的反应条件具有高对映选择性和高收率,该方法在 GPR40 受体激动剂 AMG 837 的合成中得到了应用。cod = 1,5-环辛二烯。