Author: Chatterjee, Arnab K. ; Chi, Victor ; Schultz, Peter G. ; Woods, Ashley K. ; Gebara-Lamb, Amal ; Dayan Elshan, N. G. R. ; Joseph, Sean B. ; Ghorai, Sourav ; Wilson, Katy ; Beutler, Nathan ; Li, Shuangwei ; Nazarian, Armen ; Grabovyi, Gennadii ; Weiss, Frank ; Nguyen-Tran, Vân T. B. ; Kirkpatrick, Melanie G. ; Gupta, Anil Kumar ; Liu, Yuyin ; Song, Lirui ; Wolff, Karen C. ; Malvin, Jacqueline ; Bakowski, Malina A. ; McNamara, Case W. ; Huang, Edward ; Okwor, Neechi ; Riva, Laura ; Rahimi, Alireza ; Rogers, Thomas F. ; Chen, Jian Jeffrey ; Mazumdar, Wrickban ; Pedroarena, James

There remains a need to develop novel SARS-CoV-2 therapeutic options that improve upon existing therapies by an increased robustness of response, fewer safety liabilities, and global-ready accessibility. Functionally critical viral main protease (M^pro, 3CL^pro) of SARS-CoV-2 is an attractive target due to its homology within the coronaviral family, and lack thereof toward human proteases. In this disclosure, we outline the advent of a novel SARS-CoV-2 3CL^pro inhibitor, CMX990, bearing an unprecedented trifluoromethoxymethyl ketone warhead. Compared with the marketed drug nirmatrelvir (combination with ritonavir = Paxlovid), CMX990 has distinctly differentiated potency (∼5× more potent in primary cells) and human in vitro clearance (>4× better microsomal clearance and >10× better hepatocyte clearance), with good in vitro-to-in vivo correlation. Based on its compelling preclinical profile and projected once or twice a day dosing supporting unboosted oral therapy in humans, CMX990 advanced to a Phase 1 clinical trial as an oral drug candidate for SARS-CoV-2.

01 Sep 2014·Tetrahedron Letters

3-Quinuclidinol as a nucleophilic catalyst for the cyanation of 2-chloropyrimidines

Author: Hong-Yong Kim ; Mahavir Prashad ; Wen-Chung Shieh

3-Quinuclidinol serves as an effective nucleophilic catalyst for the preparation of 2-cyanopyrimidines by cyanation of 2-chloropyrimidines with potassium cyanide in good yields.

3-Quinuclidinol

Author: Leahy, Ellen M.

A review.Properties and use of 3-quinuclidinol as a catalyst for Baylis-Hillman and aza-Baylis-Hillman, α-iodination and cyanation reactions as well as a reagent in the cleavage of β-keto esters and branched aldehydes are reviewed.

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Indication	Highest Phase	Country/Location	Organization	Date
SARS-CoV-2 acute respiratory disease	Preclinical	United States	La Jolla Pharmaceutical Co.	09 Feb 2024

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