Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
Frontier Science Center for Transformative Molecules, School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
Chemistry. 2022 Aug 4;28(44):e202201517. doi: 10.1002/chem.202201517. Epub 2022 Jun 20.
The azole-directed cobalt-catalyzed asymmetric hydrogenation of alkenes has been developed with high efficiency. With this approach, chiral pyrazole compounds were obtained in quantitative yields and excellent enantioselectivities (up to 99 % ee) under mild conditions, and the hydrogenation was conducted on a gram scale with up to 2000 TON. Several useful applications were demonstrated including the convenient introduction of β-chirality to a drug intermediate containing an azole ring.
已开发出高效的唑定向钴催化烯烃不对称氢化方法。在此方法中,在温和条件下以定量产率和优异的对映选择性(高达 99%ee)获得手性吡唑化合物,并且在高达 2000 TON 的规模上进行氢化。已经证明了几种有用的应用,包括方便地将β-手性引入含有唑环的药物中间体中。