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From Chiral Resolution to Ellman Chemistry to Biocatalysis

有机合成与工艺文献分享 2025-03-22 07:19
文章摘要
本文探讨了在有机合成中，如何通过手性拆分、Ellman化学和生物催化技术来合成具有挑战性的中间体。研究首先通过改进的路线，利用非对映选择性的Ellman亚磺酰亚胺还原作为手性胺合成的关键步骤。随后，研究还探索了使用胺转氨酶（ATA）生物催化反应来合成N-Boc酮前体的方法，该方法在亚千克规模上展示了其潜力，并因其在合成效率、总收率和过程绿色性方面的显著改进，有望成为后期临床和商业化的路线。尽管在起始材料N-Boc酮15的合成中尝试了替代路线，但效果有限。
From Chiral Resolution to Ellman Chemistry to Biocatalysis
查看文献： From Chiral Resolution to Diastereoselective Ellman Chemistry to Biocatalysis: Route Evolution for the Efficient Synthesis of the Tetrahydrobenzoazepine Core of BTK Inhibitor BIIB091
查看期刊： Organic Process Research & Development
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