Evolution of a Scale-Up Synthesis to a Potent GluN2B Inhibitor and Its Prodrug-Reference-Cited by-同舟云学术

Evolution of a Scale-Up Synthesis to a Potent GluN2B Inhibitor and Its Prodrug

Published:2018-06-05 Issue:7 Volume:22 Page:846-855
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Kempson James¹^ORCID,Zhang Huiping¹,Wong Michael K. Y.¹,Li Jianqing¹^ORCID,Li Peng¹,Wu Dauh-Rurng¹,Rampulla Richard¹,Galella Michael A.²,Dabros Marta²,Traeger Sarah C.¹,Muthalagu Vetrichelvan³,Gupta Anuradha³,Arunachalam Pirama Nayagam³,Mathur Arvind¹

Affiliation:

1. Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, Princeton, New Jersey 08540, United States

2. Drug Product Science & Technology, Materials Science & Engineering, Bristol-Myers Squibb Research and Development, Princeton, New Jersey 08540, United States

3. Department of Discovery Synthesis, Biocon Bristol-Myers Squibb Research Center (BBRC), Bangalore 560099, India

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.8b00120

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3. bThompson, L. A., III; Macor, J. E. (Bristol-Myers Squibb Company, Princeton, NJ, USA). (R)-3-((3S,4S)-3-Fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders. U.S. Pat. Appl. Pub. US 20150191496 A1, 2015.

4. Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder

5. BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder

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