A Synthesis of a Spirocyclic Macrocyclic Protease Inhibitor for the Treatment of Hepatitis C.
Org Lett
; 18(6): 1394-7, 2016 Mar 18.
Article
em En
| MEDLINE
| ID: mdl-26950496
ABSTRACT
The development of a convergent and highly stereoselective synthesis of an HCV NS3/4a protease inhibitor possessing a unique spirocyclic and macrocyclic architecture is described. A late-stage spirocyclization strategy both enabled rapid structure-activity relationship studies in the drug discovery phase and simultaneously served as the basis for the large scale drug candidate preparation for clinical use. Also reported is the discovery of a novel InCl3-catalyzed carbonyl reduction with household aluminum foil or zinc powder as the terminal reductant.
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Compostos de Espiro
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Hepatite C
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Proteínas não Estruturais Virais
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Hepacivirus
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Compostos Macrocíclicos
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Compostos Heterocíclicos de 4 ou mais Anéis
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article