Synthesis of Nirmatrelvir: Design and Optimization of an Efficient Telescoped Amidation–Dehydration Sequence-Reference-Cited by-同舟云学术

Synthesis of Nirmatrelvir: Design and Optimization of an Efficient Telescoped Amidation–Dehydration Sequence

Published:2023-11-17 Issue:12 Volume:27 Page:2250-2259
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Algera Russell F.¹,Baldwin Aaron F.²^ORCID,Bowles Paul¹,Clarke Hugh J.²,Connor Christina G.¹,Cordi Eric M.¹,Do Nga M.¹,Nicholson Lindsay D.¹,Georgian William¹,Happe Alan³,Herman Madeline I.¹,Hilou Elaa¹,James Chintelle¹,Johnson Amber M.¹,Kalinowski Maciej²,Kulkarni Samir A.¹,Launer-Felty Katherine D.²,Lee Johnny W.¹^ORCID,Lee Taegyo¹^ORCID,Lopez Jorge²,McInturff Emma L.¹^ORCID,Piper Jared L.¹,Place David W.¹^ORCID,Ragan John A.¹^ORCID,Rauschenberger Blake¹,Ryder Katherine²,Stanley Michael³,Weisenburger Gerald A.¹,Weekly R. Matthew¹,Allais Christophe¹^ORCID

Affiliation:

1. Pfizer Chemical Research and Development, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States

2. Analytical Research and Development, Pfizer Worldwide Research and Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, United States

3. Pfizer Chemical Research and Development, Process Development Facility, Pfizer Worldwide Research and Development, Discovery Park, Sandwich, Kent CT13 9NJ, United Kingdom

Funder

Pfizer

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.3c00250

Reference27 articles.

1. An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

2. aWu, G.; Chen, F. X.; Rashatasakhon, P.; Eckert, J. M.; Wong, G. S.; Lee, H.C.; Erickson, N. C.; Vance, J. A.; Nirchio, P. C.; Weber, J.; Tsai, J.S.; Zou, N.; Schering Corporation. Process for the Preparation of 6, 6-Dimethyl-3-Azabicyclo-[3.1.0]-hexane Compounds and Enantiomeric Salts Thereof. Patent WO2007075790, 2007.

3. Efficient, Chemoenzymatic Process for Manufacture of the Boceprevir Bicyclic [3.1.0]Proline Intermediate Based on Amine Oxidase-Catalyzed Desymmetrization

4. Synthesis of Nirmatrelvir: Development of a Scalable Cobalt-Catalyzed Cyclopropanation for Manufacture of the Bicyclic [3.1.0]Proline-Building Block

5. Early Clinical Development of Lufotrelvir as a Potential Therapy for COVID-19

Cited by 3 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Synthesis of Nirmatrelvir: Development of a Scalable Cobalt-Catalyzed Cyclopropanation for Manufacture of the Bicyclic [3.1.0]Proline-Building Block;Organic Process Research & Development;2023-12-04

2. Synthesis of Nirmatrelvir: Development of an Efficient, Scalable Process to Generate the Western Fragment;Organic Process Research & Development;2023-11-25

3. Synthesis of Nirmatrelvir: Development of Magnesium Sulfate-Mediated Aminolysis for the Manufacture of the Eastern Fragment;Organic Process Research & Development;2023-11-22