Enantioselective bioreduction for the preparation of integrin receptor antagonist intermediates

The present invention relates to a bioreductive process for the efficient preparation of chiral allylic alcohol intermediates which are useful in the asymmetric synthesis of integrin v 3 receptor antagonists. The process comprises an enantioselective 1,2-reduction of a prochiral , -unsaturated keton...

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Bibliographische Detailangaben
Hauptverfasser: Sturr, Michael G, Boyd, Russell Fieldon, Gbewonyo, Kodzo, Nti-Gyabaah, Joseph, Pollard, David J, McWilliams, James Christopher, Telari, Kathleen A
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention relates to a bioreductive process for the efficient preparation of chiral allylic alcohol intermediates which are useful in the asymmetric synthesis of integrin v 3 receptor antagonists. The process comprises an enantioselective 1,2-reduction of a prochiral , -unsaturated ketone using a yeast microorganism to afford a chiral allylic alcohol which can be further processed into the desired substituted nonanoic acid derivative, which is useful as an integrin v 3 receptor antagonist for the inhibition of bone resorption and treatment of osteoporosis. The present invention relates to a novel enantioselective bioreduction using a yeast microorganism for the preparation of the chiral allylic alcohols of structural formula I (R is hydrogen or methyl) which are useful in the asymmetric synthesis of integrin v receptor antagonists.