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Synthesis of Nirmatrelvir: Design and Optimization of an Efficient Telescoped Amidation–Dehydration Sequence
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2023-11-17 , DOI: 10.1021/acs.oprd.3c00250 Russell F. Algera 1 , Aaron F. Baldwin 2 , Paul Bowles 1 , Hugh J. Clarke 2 , Christina G. Connor 1 , Eric M. Cordi 1 , Nga M. Do 1 , Lindsay D. Nicholson 1 , William Georgian 1 , Alan Happe 3 , Madeline I. Herman 1 , Elaa Hilou 1 , Chintelle James 1 , Amber M. Johnson 1 , Maciej Kalinowski 2 , Samir A. Kulkarni 1 , Katherine D. Launer-Felty 2 , Johnny W. Lee 1 , Taegyo Lee 1 , Jorge Lopez 2 , Emma L. McInturff 1 , Jared L. Piper 1 , David W. Place 1 , John A. Ragan 1 , Blake Rauschenberger 1 , Katherine Ryder 2 , Michael Stanley 3 , Gerald A. Weisenburger 1 , R. Matthew Weekly 1 , Christophe Allais 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2023-11-17 , DOI: 10.1021/acs.oprd.3c00250 Russell F. Algera 1 , Aaron F. Baldwin 2 , Paul Bowles 1 , Hugh J. Clarke 2 , Christina G. Connor 1 , Eric M. Cordi 1 , Nga M. Do 1 , Lindsay D. Nicholson 1 , William Georgian 1 , Alan Happe 3 , Madeline I. Herman 1 , Elaa Hilou 1 , Chintelle James 1 , Amber M. Johnson 1 , Maciej Kalinowski 2 , Samir A. Kulkarni 1 , Katherine D. Launer-Felty 2 , Johnny W. Lee 1 , Taegyo Lee 1 , Jorge Lopez 2 , Emma L. McInturff 1 , Jared L. Piper 1 , David W. Place 1 , John A. Ragan 1 , Blake Rauschenberger 1 , Katherine Ryder 2 , Michael Stanley 3 , Gerald A. Weisenburger 1 , R. Matthew Weekly 1 , Christophe Allais 1
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Development of a scalable route for the synthesis of nirmatrelvir, the novel SARS-CoV-2 3C-like protease inhibitor discovered in 2020 by Pfizer scientists, was initiated shortly thereafter to supply material for the first clinical studies. This route was optimized for commercial manufacture of nirmatrelvir in high yield and acceptable quality with consideration of efficiency and sustainability. Herein, we report the evolution of final steps (3–5) used to synthesize nirmatrelvir (steps 3–5), from the manufacture of the initial regulatory lot to the design and implementation of the final commercial process.
中文翻译：
Nirmatrelvir 的合成：高效伸缩式酰胺化-脱水序列的设计和优化
此后不久，辉瑞科学家于 2020 年发现了 nirmatrelvir（一种新型 SARS-CoV-2 3C 样蛋白酶抑制剂）合成可扩展路线的开发，为首次临床研究提供材料。考虑到效率和可持续性，该路线经过优化，可实现高产率和可接受的质量的尼马曲韦商业化生产。在此，我们报告了用于合成 nirmatrelvir（步骤 3-5）的最终步骤 (3-5) 的演变，从初始监管批次的制造到最终商业流程的设计和实施。
更新日期：2023-11-17
中文翻译：
Nirmatrelvir 的合成：高效伸缩式酰胺化-脱水序列的设计和优化
此后不久，辉瑞科学家于 2020 年发现了 nirmatrelvir（一种新型 SARS-CoV-2 3C 样蛋白酶抑制剂）合成可扩展路线的开发，为首次临床研究提供材料。考虑到效率和可持续性，该路线经过优化，可实现高产率和可接受的质量的尼马曲韦商业化生产。在此，我们报告了用于合成 nirmatrelvir（步骤 3-5）的最终步骤 (3-5) 的演变，从初始监管批次的制造到最终商业流程的设计和实施。
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