Biocatalytic approaches to a key building block for the anti-thrombotic agent ticagrelor

Research output: Contribution to journalArticle

  • Authors:
  • Katharina G. Hugentobler
  • Humera Sharif
  • Marcello Rasparini
  • Rachel S. Heath
  • Nicholas J. Turner

Abstract

Three complementary biocatalytic routes were examined for the synthesis of the cyclopropyl amine (1R,2S)-2, which is a key building block for the anti-thrombotic agent ticagrelor 1. By employing either a ketoreductase, amidase or lipase biocatalyst, the key building blocks for synthesis of the amine 2 were obtained in 99.9, 92.5 and 46.3 ee, respectively.

Bibliographical metadata

Original languageEnglish
Pages (from-to)8064-8067
Number of pages4
JournalOrganic and Biomolecular Chemistry
Volume14
Issue number34
Early online date25 Jul 2016
DOIs
StatePublished - 2016