Azole-Directed Cobalt-Catalyzed Asymmetric Hydrogenation of Alkenes

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 beta-chirality to a drug intermediate containing an azole ring.

Automated summary

A highly efficient azole-directed cobalt-catalyzed asymmetric hydrogenation of alkenes has been developed. This method allows for the synthesis of chiral pyrazole compounds with quantitative yields and excellent enantioselectivities (up to 99% ee) under mild conditions. The reaction can be conducted on a gram scale with high turnover numbers (up to 2000 TON) and has demonstrated several useful applications including the introduction of beta-chirality to drug intermediates containing an azole ring.