Development of a Robust Manufacturing Route for Molnupiravir, an Antiviral for the Treatment of COVID-19

被引：17

作者：

Fier, Patrick S. ^{[1
]}

Xu, Yingju ^{[1
]}

Poirier, Marc ^{[1
]}

Brito, Gilmar ^{[1
]}

Zheng, Michelle ^{[1
]}

Bade, Rachel ^{[1
]}

Sirota, Eric ^{[1
]}

Stone, Kevin ^{[1
]}

Tan, Lushi ^{[1
]}

Humphrey, Guy R. ^{[1
]}

Chang, Darryl ^{[1
]}

Bothe, Jameson ^{[1
]}

Zhang, Yongqian ^{[1
]}

Bernardoni, Frank ^{[1
]}

Castro, Steve ^{[1
]}

Zompa, Michael A. ^{[1
]}

Taylor, Jerry ^{[1
]}

Sirk, Kevin M. ^{[1
]}

Diaz-Santana, Anthony ^{[1
]}

Diribe, Ike ^{[1
]}

Emerson, Khateeta M. ^{[1
]}

Krishnamurthi, Bharath ^{[1
]}

Zhao, Ralph ^{[1
]}

Ward, Michael ^{[1
]}

Xiao, Chengqian ^{[2
]}

Ouyand, Honggui ^{[2
]}

Zhan, Jianfeng ^{[2
]}

Morris, William J. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Proc Res & Dev, Rahway, NJ 07065 USA

[2] WuXi AppTec Co Ltd, Shanghai 200131, Peoples R China

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2021年 / 25卷 / 12期

关键词：

molnupiravir; covid-19; antiviral; crystallization; DERIVATIVES;

D O I：

10.1021/acs.oprd.1c00400

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Herein is described the development of a large-scale manufacturing process for molnupiravir, an orally dosed antiviral that was recently demonstrated to be efficacious for the treatment of patients with COVID-19. The yield, robustness, and efficiency of each of the five steps were improved, ultimately culminating in a 1.6-fold improvement in overall yield and a dramatic increase in the overall throughput compared to the baseline process.

引用

页码：2806 / 2815

页数：10

共 50 条

[1] Antiviral Efficacy of Molnupiravir for COVID-19 Treatment
Bai, Yuan
Shen, Mingwang
Zhang, Lei
[J]. VIRUSES-BASEL, 2022, 14 (04):
[2] Molnupiravir: an antiviral drug against COVID-19
Bhavarth Dave
Kashvi C. Shah
Mehul R. Chorawala
Nirav Shah
Pranjal Patel
Suzan Patel
Palak Shah
[J]. Archives of Virology, 2023, 168
[3] Covid-19: What is the evidence for the antiviral molnupiravir?
Extance, Andy
[J]. BMJ-BRITISH MEDICAL JOURNAL, 2022, 377
[4] Molnupiravir: an antiviral drug against COVID-19
Dave, Bhavarth
Shah, Kashvi C.
Chorawala, Mehul R.
Shah, Nirav
Patel, Pranjal
Patel, Suzan
Shah, Palak
[J]. ARCHIVES OF VIROLOGY, 2023, 168 (10)
[5] Molnupiravir for the treatment of COVID-19
Santani, Bela G.
LeBlanc, Brian W.
Thakare, Ritesh P.
[J]. DRUGS OF TODAY, 2022, 58 (07) : 335 - 350
[6] Molnupiravir for Treatment of COVID-19
不详
[J]. MEDICAL LETTER ON DRUGS AND THERAPEUTICS, 2022, 64 (1642): : 10 - 11
[7] Repurposing Molnupiravir for COVID-19: The Mechanisms of Antiviral Activity
Yip, Ashley Jia Wen
Low, Zheng Yao
Chow, Vincent T. K.
Lal, Sunil K.
[J]. VIRUSES-BASEL, 2022, 14 (06):
[8] Molnupiravir and Its Antiviral Activity Against COVID-19
Tian, Lili
Pang, Zehan
Li, Maochen
Lou, Fuxing
An, Xiaoping
Zhu, Shaozhou
Song, Lihua
Tong, Yigang
Fan, Huahao
Fan, Junfen
[J]. FRONTIERS IN IMMUNOLOGY, 2022, 13
[9] Polymorphs, Particle Size, and a Pandemic: Development of a Scalable Crystallization Process for Molnupiravir, an Antiviral for the Treatment of COVID-19
Bade, Rachel
Bothe, Jameson R.
Sirota, Eric
Brunskill, Andrew P. J.
Newman, Justin A.
Zhang, Yongqian
Tan, Melissa
Zheng, Michelle
Brito, Gilmar
Poirier, Marc
Fier, Patrick S.
Xu, Yingju
Ward, Michael D.
Stone, Kevin
Lee, Ivan H.
Gmitter, Andrew J.
Bernardoni, Frank
Zompa, Michael A.
Luo, Hanlin
Patel, Sanjaykumar
Masiuk, Tina
Mora, Jeff
Ni, Tong
Okoh, Grace A.
Tarabokija, James
Liu, Jiaying
Lowinger, Michael B.
Mahmood, Tariq
[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023, 27 (11) : 2100 - 2110
[10] Molnupiravir: A new candidate for COVID-19 treatment
Pourkarim, Fariba
Pourtaghi-Anvarian, Samira
Rezaee, Haleh
[J]. PHARMACOLOGY RESEARCH & PERSPECTIVES, 2022, 10 (01):

← 1 2 3 4 5 →