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.

中文翻译：

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一种可扩展的替代5取代的3-异恶唑醇纤溶抑制剂AZD6564的途径

从2-氯异烟酸甲酯开始，共分八步开发了实用且无色谱的包含3-异恶唑醇的抗纤维蛋白溶解剂AZD6564的多千克合成方法，总产率为7％。合成中的重点是Negishi偶联和外消旋酯的酶促拆分。