An Improved and Scalable Process for the Synthesis of Ezetimibe: An Antihypercholesterolemia Drug†

…, P Reddy Padi, V Sunkara, P Ramayya…

Index: Sasikala; Padi, Pratap Reddy; Sunkara, Vishnuvardhan; Ramayya, Pattabhi; Dubey; Uppala, Venkata Bhaskar Rao; Praveen, Cherukupally Organic Process Research and Development, 2009 , vol. 13, # 5 p. 907 - 910

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Citation Number: 27

Abstract

An efficient, cost-effective and large-scale synthesis of ezetimibe 1, an antihypercholesterolemia drug, is described. Chiral oxazolidinone chemistry was used to fix the required stereochemistry of the β-lactam ring, and the chiral oxazaborolidine chemistry was used to fix the hydroxyl group stereochemistry. The synthesis significantly lowers the cost and provides easy access to ezetimibe on large scale.

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