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P. 40-43 /

The asymmetric hydrogenation of heterocyclic ketones

ANTONIO ZANOTTI-GEROSA1, ANDREAS MARC PALMER2
1. Johnson Matthey, Catalysis and Chiral Technologies, 28 Cambridge Science Park, Cambridge, CB4 05P, United Kingdom
2. Nycomed GmbH, Dep. of Medicinal Chemistry, Byk-Gulden-Str.2, Konstanz, D-78467, Germany

Abstract

Potassium-competitive acid blockers (P-CABs)containing an imidazo[1,2-a]pyridine / benzimidazole scaffold,respectively were prepared via asymmetric hydrogenationof aryl ketone intermediates in the presence of RuCl2[(S)-Xyl-P-Phos][(S)-DAIPEN]. The enantioselective synthesis of BYK405879 was successfully implemented on Kg scale.


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