op500193s_si_001.pdf (934.49 kB)
A Scalable Route to 5‑Substituted 3‑Isoxazolol Fibrinolysis Inhibitor AZD6564
journal contribution
posted on 2014-08-15, 00:00 authored by Søren
M. Andersen, Martin Bollmark, Robert Berg, Christofer Fredriksson, Staffan Karlsson, Catarina Liljeholm, Henrik SörensenA 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.
