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A scalable route to 5-substituted 3-isoxazolol fibrinolysis inhibitor AZD6564
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- Andersen, Sören M. (author)
- Novo Nordisk A/S, Denmark
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- Bollmark, Martin (author)
- RISE,Substans och formulering
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- Berg, Robert (author)
- RISE,Katalys
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- (creator_code:org_t)
- 2014-08-06
- 2014
- English.
- In: Organic Process Research & Development. - : American Chemical Society (ACS). - 1083-6160 .- 1520-586X. ; 18:8, s. 952-959
- Journal article (peer-reviewed)
Abstract
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- A practical and chromatography-free multikilogram synthesis of a 3-isoxazolol containing antifibrinolytic agent, AZD6564, has been developed in eight steps and 7% overall yield starting from methyl 2-chloroisonicotinate. Highlights in the synthesis are a Negishi coupling and an enzymatic resolution of a racemic ester.
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