Asymmetric alkynylation of thiazolones and azlactones with alkynylbenziodoxolones as the electrophilic alkyne source catalyzed by thiourea phosphonium salt is described. By using thiazolones as nucleophiles, the desired alkyne functionalized thiazolones were obtained in 55–89% yields with 31–86% ee. Azlactones gave the desired products in comparable yields with lower enantioselectivities. Ring-opening
描述了硫脲鏻盐催化的噻唑酮和吖内酯的不对称炔基化反应,其中炔基苯并氧唑酮作为亲电炔烃源。通过使用噻唑酮作为亲核试剂,以 55-89% 的产率和 31-86% 的 ee 获得所需的炔烃官能化噻唑酮。Azlactones 以较低的对映选择性以相当的产率得到所需的产物。炔基化产物的开环导致α,α-二取代的α-氨基酸衍生物有效而不会损失对映选择性。