We report on the covalent immobilization of the (S)‐selective amine transaminase from Vibrio fluvialis (Vf‐ATA) and its use in the synthesis of (S)‐1‐(5‐fluoropyrimidin‐2‐yl)‐ethanamine, a key intermediate of the JAK2 kinase inhibitor AZD1480. Immobilized Vf‐ATA on glyoxyl‐agarose (activity recovery: 30 %) was used in a packed‐bed reactor to set‐up a continuous flow biotransformation coupled with a straightforward in‐line purification to circumvent the 2‐step process described in literature for the batch reaction. The newly developed biotransformation was run in a homogeneous system including dimethyl carbonate as a green co‐solvent. Optically pure (S)‐1‐(5‐fluoropyrimidin‐2‐yl)‐ethanamine (ee >99 %) was isolated in 35 % yield.

中文翻译：

---

在流动条件下使用固定化的来自河流弧菌的氨基转氨酶合成（S）-1-（5-氟代嘧啶-2-2-基）-乙胺

我们报道了来自弧菌（Vf- ATA）的（S）-选择性胺转氨酶的共价固定化及其在（S）-1-（5-氟嘧啶-2-2-基）-乙胺的合成中的应用JAK2激酶抑制剂AZD1480的中间体。在填充床反应器中使用固定在乙醛琼脂糖上的Vf -ATA（活性回收率：30％）进行连续流生物转化，并进行直接在线纯化，以规避文献中所述的两步法分批反应。新开发的生物转化系统在均质系统中运行，其中包括碳酸二甲酯作为绿色助溶剂。光学纯（S）1-（5-氟嘧啶-2-基）乙胺（ee> 99％）的分离产率为35％。