Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264). Part 5: Completion of the API Free Base via a Direct Chlorosulfonylation Process
Author:
Affiliation:
1. Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry,Physical and Theoretical Chemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.0c00247
Reference28 articles.
1. Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 3: Development of a One-Pot Formylation–Cyclization Sequence to the Diaminopyrimidine Core
2. Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 4: Formylation–Cyclization as a Flow–Batch Process Leads to Significant Improvements in Process Mass Intensity (PMI) and CO Generated versus the Batch–Batch Process
3. ICH Q3C Impurities: Guideline for Residual Solvents (R6). https://database.ich.org/sites/default/files/Q3C-R6_Guideline_ErrorCorrection_2019_0410_0.pdf (accessed Nov 26, 2019).
4. Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 1: Introduction and Process Overview
5. Molecular design and synthesis of HCV inhibitors based on thiazolone scaffold
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2. Challenges with retention and recovery of impurities containing acidic moieties during analytical UHPLC method development and validation for gefapixant freebase;Journal of Pharmaceutical and Biomedical Analysis;2024-01
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4. Gefapixant Citrate (MK-7264) Sulfonamide Step Speciation Study: Investigation into Precipitation–Dissolution Events during Addition of Chlorosulfonic Acid;Organic Process Research & Development;2023-02-08
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