The first general palladium catalyst for the Suzuki-Miyaura and carbonyl enolate coupling of aryl arenesulfonates

Authors

Cliff C. Cheng, Merck & Co., Inc.
Xiaohua Huang, Merck & Co., Inc.
Gerald W. Shipps, Merck & Co., Inc.
Yu Sen Wang, Merck & Co., Inc.
Daniel F. Wyss, Merck & Co., Inc.
Kyle A. Soucy, Merck & Co., Inc.
Chuan Kui Jiang, Merck & Co., Inc.
Sony Agrawal, Merck & Co., Inc.
Eric Ferrari, Merck & Co., Inc.
Zhiqing He, Merck & Co., Inc.
H. C. Huang, Merck & Co., Inc.

Abstract

Pyridine carboxamide-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified and optimized to a variety of topologically related scaffolds. In particular, the 2-methyl nicotinic acid scaffold was developed into inhibitors with improved biochemical (IC50-GT1b = 0.014 μM) and cell-based HCV replicon potency (EC50-GT1b = 0.7 μM). Biophysical and biochemical characterization identified this novel series of compounds as palm site binders to HCV polymerase. © 2010 American Chemical Society.

Publication Title

Journal of the American Chemical Society

Recommended Citation

Cheng, C., Huang, X., Shipps, G., Wang, Y., Wyss, D., Soucy, K., Jiang, C., Agrawal, S., Ferrari, E., He, Z., & Huang, H. (2003). The first general palladium catalyst for the Suzuki-Miyaura and carbonyl enolate coupling of aryl arenesulfonates. Journal of the American Chemical Society, 125 (39), 11818-11819. https://doi.org/10.1021/ja036947t