ABSTRACT
An enantiopure piperidine, a key intermediate for the synthesis of (+)-tofacitinib, has been achieved in high optical purity (98% ee) from readily available crotyl alcohol. The key steps involved is a CoIII(salen)-OAc-catalyzed two stereocentered hydrolytic kinetic resolution of (±)-methyl-3-(oxiran-2-yl)butanoate.
GRAPHICAL ABSTRACT
Acknowledgments
Rohit B. Kamble thanks CSIR (National Repository of Small Molecules) for providing fellowship and DST-SERB, New Delhi for funds. The authors are also thankful to Dr. S. S. Tambe, Chair, Chemical Engineering and Process Development Division for his constant encouragement and support.