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Issue 34, 2016
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Biocatalytic approaches to a key building block for the anti-thrombotic agent ticagrelor

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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.

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

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Article information


Submitted
26 Jun 2016
Accepted
25 Jul 2016
First published
25 Jul 2016

Org. Biomol. Chem., 2016,14, 8064-8067
Article type
Paper
Author version available

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

K. G. Hugentobler, H. Sharif, M. Rasparini, R. S. Heath and N. J. Turner, Org. Biomol. Chem., 2016, 14, 8064
DOI: 10.1039/C6OB01382A

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