A Synthesis of a Spirocyclic Macrocyclic Protease Inhibitor for the Treatment of Hepatitis C.
Org Lett
; 18(6): 1394-7, 2016 Mar 18.
Article
in 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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Spiro Compounds
/
Hepatitis C
/
Viral Nonstructural Proteins
/
Hepacivirus
/
Macrocyclic Compounds
/
Heterocyclic Compounds, 4 or More Rings
Language:
En
Journal:
Org Lett
Journal subject:
BIOQUIMICA
Year:
2016
Document type:
Article
Affiliation country:
United States