Add time:09/02/2019         Source:sciencedirect.com

A straightforward chemoenzymatic synthesis of Rasagiline (cas 136236-51-6) mesylate has been developed. The key steps for the introduction of chirality involved kinetic enzymatic resolution with lipases via acetylation of rac-indanol and an inversion configuration Mitsunobu reaction of the produced (S)-indanol. Immobilized lipase from Thermomyces lanuginosus proved to be a robust biocatalyst in the kinetic resolution, leading to (S)-indanol with high selectivity (e.e. > 99%, E > 200) in just 15 min, at 35 °C, in hexane, being reused for ten-times without significant loss of the activity and selectivity.

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