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

doi:10.1039/c6ob01382a

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^*

^*Corresponding author for this work

The University of Manchester

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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 language	English
Pages (from-to)	8064-8067
Number of pages	4
Journal	Organic and Biomolecular Chemistry
Volume	14
Issue number	34
Early online date	25 Jul 2016
DOIs	https://doi.org/10.1039/c6ob01382a
Publication status	Published - 2016

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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.",

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AU - Hugentobler, Katharina G.

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AU - Heath, Rachel S.

AU - Turner, Nicholas J.

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AB - 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.

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

Abstract

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