Zhejiang Raybow Pharmaceutical Co., Ltd. , No. 18 Nanyangsan Road , Linhai, Taizhou City , Zhejiang Province 318000 , People's Republic of China.
State Key Laboratory and Institute of Elemento-organic Chemistry, College of Chemistry , Nankai University , Tianjin 300071 , People's Republic of China.
Org Lett. 2020 Feb 7;22(3):818-822. doi: 10.1021/acs.orglett.9b04253. Epub 2020 Jan 21.
A highly efficient asymmetric hydrogenation of γ- and δ-ketoacids was developed by using a chiral spiro iridium catalyst ()-, affording the optically active γ- and δ-hydroxy acids/lactones in high yields with excellent enantioselectivities (up to >99% ee) and turnover numbers (TON up to 100000). This protocol provides an efficient and practical method for enantioselective synthesis of Ezetimibe.
手性螺环铱催化剂（）高效实现了γ-和δ-酮酸的不对称氢化反应，以高收率和优异的对映选择性（高达>99%ee）及周转数（TON 高达 100000）得到了光学活性的γ-和δ-羟基酸/内酯。该方法为依泽替米贝的对映选择性合成提供了一种有效实用的方法。
