title: Biocatalytic approaches to a key building block for the anti-thrombotic agent ticagrelor.
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.
authors.affiliation: School of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, Manchester M1 7DN, UK. Nicholas.Turner@manchester.ac.uk.
authors.forename: Katharina G
authors.initials: KG
authors.lastname: Hugentobler
authors.forename: Humera
authors.initials: H
authors.lastname: Sharif
authors.forename: Marcello
authors.initials: M
authors.lastname: Rasparini
authors.forename: Rachel S
authors.initials: RS
authors.lastname: Heath
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Turner
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000588:Amines / Q000737:chemistry; D055162:Biocatalysis; D060326:Chemistry Techniques, Synthetic; D006868:Hydrolysis; D013927:Thrombosis / Q000188:drug therapy*; D000077486:Ticagrelor
chemical_list: D000588:Amines; D000077486:Ticagrelor; D000241:Adenosine