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

Katharina G. Hugentobler, Humera Sharif, Marcello Rasparini, Rachel S. Heath, Nicholas J. Turner

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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.

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

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