Development of a Scaleable Synthesis of a Partial Nicotinic Acid Receptor Agonist

Author:

Wilson Robert D.1,Cleator Ed1,Ashwood Michael S.1,Bio Matthew M.1,Brands Karel M. J.1,Davies Antony J.1,Dolling Ulf-H.1,Emerson Khateeta M.1,Gibb Andrew D.1,Hands David1,McKeown Arlene E.1,Oliver Steven F.1,Reamer Robert A.1,Sheen Faye J.1,Stewart Gavin W.1,Zhou George X.1

Affiliation:

1. Department of Process Research, Merck Sharp and Dohme Research Laboratories, Hertford Road, Hoddesdon, Hertfordshire EN11 9BU, U.K., and Department of Process Research, Merck Research Laboratories, Rahway, New Jersey 07065, U.S.A.

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Reference10 articles.

1. Carballo-Jane, E., Richman, J. G., Cheng, K., Cai, T. Q., Taggart, A. K. P., Gaidarov, I., Cameron, J. S., Boatman, P. D., Chen, R., Semple, G., Connolly, D. T., Hammond, M., Wright, S. D., Colletti, S. L., Tata, J. R., Forrest, M. J., and Waters, M. G.Discovery and Characterization of a partial agonist of niacotinic acid receptor GPR109A.XVI International Symposium on Drugs Affecting Lipid Metabolism,New York, N.Y.,October 4−7, 2007.

2. The benefits of niacin in atherosclerosis

3. 3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A Partial Agonist of the Nicotinic Acid Receptor, G-Protein Coupled Receptor 109a, with Antilipolytic but No Vasodilatory Activity in Mice

4. Pyrazole Derivatives as Partial Agonists for the Nicotinic Acid Receptor

5. Preparation of 5-Substituted 1H-Tetrazoles from Nitriles in Water

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