用化学-酶法制备光学产率高的伊非那唑。

IF 3.3 2区 化学 Q1 CHEMISTRY, ORGANIC
Zhiran Ju, Zhiyun Li, Menglan Li, Saili Xu, Kumaravel Kaliaperumal and Fen-Er Chen*, 
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引用次数: 0

摘要

在此,我们提出了一种新的、生态友好的生物催化方法来合成临床使用的抗真菌剂烯那康唑(7)。该方法涉及利用苯甲醛裂解酶(BAL)催化酮前体中关键的安息香缩合步骤。在硫胺素二磷酸(ThDP)和Mg2+存在下,用BAL处理2,4-二氟苯甲醛,生成α-羟基酮,然后制备7。这种创新方法不仅提供了一种更环保的替代方案,而且与传统化学工艺相比具有显著优势。通过我们的努力和开发工作,我们建立了高效和可扩展的程序,使7的产量达到38%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

A Chemo-Enzymatic Approach for Preparing Efinaconazole with High Optical Yield

A Chemo-Enzymatic Approach for Preparing Efinaconazole with High Optical Yield

Herein, we present a novel and ecofriendly biocatalytic approach for synthesizing efinaconazole (7), a clinically used antifungal agent. This method involves utilizing benzaldehyde lyase (BAL) to catalyze the crucial benzoin condensation step in the ketone precursor. Treating 2,4-difluorobenzaldehyde with BAL in the presence of thiamin-diphosphate (ThDP) and Mg2+ resulted in the formation of α-hydroxy ketone which then underwent the preparation of 7. This innovative approach not only provides a greener alternative but also offers significant advantages over the traditional chemical process. Through our efforts and development work, we have established efficient and scalable procedures that enable the production of 7 in a moderate 38% yield.

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来源期刊
Journal of Organic Chemistry
Journal of Organic Chemistry 化学-有机化学
CiteScore
6.20
自引率
11.10%
发文量
1467
审稿时长
2 months
期刊介绍: Journal of Organic Chemistry welcomes original contributions of fundamental research in all branches of the theory and practice of organic chemistry. In selecting manuscripts for publication, the editors place emphasis on the quality and novelty of the work, as well as the breadth of interest to the organic chemistry community.
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