Medicines Ezetimibe

Clader, J. From Serendipity to Design The Discovery of Ezetimibe and Other Novel Cholesterol Absorption Inhibitors. Presented at Residential School on Medicinal Chemistry, Drew University, Madison, NJ, June 2002,... 

Nor are the contributions to be made by p-lactam structures to the pharmaceuticals field over. The extraordinary developments of recent years in cholesterol absorption inhibitors (CAIs) based on the p-lactam ring deserve some mention, especially since Dr. T. K. Thiruvengadam in our chemical process development organization in Schering-Plough is the brilliant architect of one of the patented syntheses of this novel class of CAIs. His synthesis35 of Ezetimibe (Zetia), outlined in Scheme 13, serves to (a) introduce this new direction in the development of novel p-lactam medicinals and (b) end this excursion in the field of p-lactams. 

Taylor, A.J., Villines, T.C., Stanek, E.J., Devine, P.J., Griffen, L., Miller, M., Weissman, N.J., and Turco, M., 2009. Extended-release niacin or ezetimibe and carotid intima-media thickness. The New England Journal of Medicine. 361 2113-2122. 

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