A Scalable Route to 5-Substituted 3-Isoxazolol Fibrinolysis Inhibitor AZD6564

Søren Andersen, Martin Bollmark, Christofer Fredriksson, Staffan Karlsson, Catarina Liljeholm, Henrik Toft Sørensen

Organic Process Research & Development · 2014 · 23 citations · 16 references

Concepts

Abstract

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.

References

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