29481-26-3

Upstream product

• 7283-96-7 5-Chloro-2-thiophenecarboxaldehyde 
• 1065010-87-8 potassium cyclopropyltrifluoroborate 
• 4701-17-1 5-bromo-2-thiophencarboxaldehyde 
• 411235-57-9 cyclopropylboronic acid 

Relevant academic research and scientific papers

Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms

We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. This NS5A inhibitor contains a unique tetracyclic indole core while maintaining the imidazole-proline-valine Moc motifs of our previous NS5A inhibitors. Compound 40 is currently in early clinical trials and is under evaluation as part of an all-oral DAA regimen for the treatment of chronic HCV infection.

SUBSTITUTED PYRIDINONES AS MGAT2 INHIBITORS

The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

THIOPHENE- SUB STITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

Disclosed are novel Thiophene-Subsituted Tetracyclic Compounds of Formula (I). And pharmaceutically acceptable salts thereof, wherein A, A', R2, R3, R4 and R5 are as defined herein. The compositions comprising at least one Thiophene-Subsituted Tetracyclic Compounds, and methods of using the Thiophene-Subsituted Tetracyclic Compounds for treating or preventing HCV infection in a patient are also disclosed.

THIOPHENE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES

Thiophene-substituted tetracyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A, A', R2, R3, R4 and R5 are as defined herein. The compositions comprising at least one thiophene-substituted tetracyclic compound, and methods of using the thiophene-substituted tetracyclic compounds for treating or preventing HCV infection in a patient are also provided.

Cross-coupling of cyclopropyl- and cyclobutyltrifluoroborates with aryl and heteroaryl chlorides

(Chemical Equation Presented) Suitable conditions were found for the Suzuki-Miyaura cross-coupling reaction of potassium cyclopropyl-and cyclobutyltrifluoroborates with aryl chlorides. Both of these secondary alkyl trifluoroborates coupled in moderate to excellent yield with electron-rich, electron-poor, and hindered aryl chlorides to give a variety of substituted aryl cyclopropanes and cyclobutanes.