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通过脂肪酶催化剂简化莫努匹拉韦的化学酶法合成。

Streamlined Chemo-Enzymatic Synthesis of Molnupiravir via Lipase Catalyst.

作者信息

Rosangzuala Khawlhring, Patlolla Ravinder Reddy, Shaikh Asif, Naik Kethavath Anjali Priya, Raveena Gajjala, Nemali Manjula, Reddy Mudiam Mohana Krishna, Banoth Linga

机构信息

Academy of Scientific and Innovative Research, Ghaziabad 201002, India.

Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India.

出版信息

ACS Omega. 2024 Jan 17;9(4):4423-4428. doi: 10.1021/acsomega.3c06872. eCollection 2024 Jan 30.

Abstract

An enzymatic approach for the synthesis of Molnupiravir has been developed using immobilized lipase as a biocatalyst. This method involves a concise process of the regioselective esterification of uridine with isobutyric anhydride using Lipase (Addzyme-011). This efficient route gets 97% conversion of uridine , with an overall 73% yield of molnupiravir in two steps. The use of inexpensive and easily available lipase makes the synthesis cost-effective and accessible globally, promoting the principles of green chemistry.

摘要

已开发出一种使用固定化脂肪酶作为生物催化剂合成莫努匹拉韦的酶促方法。该方法涉及使用脂肪酶(Addzyme - 011)将尿苷与异丁酸酐进行区域选择性酯化的简洁过程。这条高效路线使尿苷的转化率达到97%,两步反应中莫努匹拉韦的总产率为73%。使用廉价且易于获得的脂肪酶使合成具有成本效益且在全球范围内可行,符合绿色化学原则。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e699/10831972/6469cbb2c089/ao3c06872_0001.jpg

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