477558-79-5Relevant articles and documents
Azetidinone derivatives and its preparation method and application
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Paragraph 0058; 0059, (2017/03/28)
The invention discloses azacyclobutanone derivatives which are compounds as shown in the formula (I) and medicinal salts thereof. The invention further discloses a preparation method and application of the azacyclobutanone derivatives. The azacyclobutanone derivatives disclosed by the invention can be used for treating or preventing atherosclerosis or lowering plasma cholesterol level, and has strong plasma cholesterol reducing activity and wide market prospect.
An improved and scalable process for the synthesis of ezetimibe: An antihypercholesterolemia drug
Sasikala,Padi, Pratap Reddy,Sunkara, Vishnuvardhan,Ramayya, Pattabhi,Dubey,Uppala, Venkata Bhaskar Rao,Praveen, Cherukupally
experimental part, p. 907 - 910 (2010/04/22)
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.
PREPARATION OF EZETIMIBE
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Page/Page column 9, (2010/11/26)
A process for preparing ezetimibe.