Improved Synthesis and Determination of the Biologically Active Diastereomer of YK11

Abstract

The palladium catalyzed carbonylation of 1 using the chiral ligand L1 afforded 2 in a highly diastereoselective manner. The stereochemistry of the major diastereomer 2a was determined by X-ray crystallographic analysis. AR luciferase reporter assay studies suggested that 2a was the active constituent of YK11 (2).

Keywords

• YK11
• SARMs
• palladium
• carbonylation
• orthoester