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One-Pot Ketoreductase/Transaminase Process

有机合成与工艺文献分享 2025-09-06 10:15
文章摘要
背景：辉瑞团队开发了一种一锅法连续级联反应，用于合成手性二取代四氢吡喃70，以替代初始药物化学递送中使用的五步合成法。研究目的：通过酮还原酶（KRED）和转氨酶的双酶解决方案，实现外消旋酮rac-68的直接胺化和拆分，生成目标胺70，并通过Boc保护得到最终产物71。结论：该工艺在克级规模上成功筛选出商业酶，并在多公斤级放大时改用CRO专有酶以降低成本，但需要更高酶载量和中间酶去除步骤以避免乳液问题。
One-Pot Ketoreductase/Transaminase Process
查看文献： Ketoreductase/Transaminase, One-Pot, Multikilogram Biocatalytic Cascade Reaction
查看期刊： Organic Process Research & Development
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