ChemInform Abstract: Application of Epimerization-Free Amide Coupling Conditions to the Synthesis of Matrix Metalloprotease Inhibitor Intermediates.

✍ Scribed by M. J. FRAY; D. ELLIS

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 29 KB
• Volume: 30
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199911221

✦ Synopsis

Application of Epimerization-Free Amide Coupling Conditions to the Synthesis of Matrix Metalloprotease Inhibitor Intermediates.

-The tert-leucine derivative (I) is successfully coupled with a variety of amines to give peptides in good to excellent yields with minimal epimerization at the tert-leucine stereogenic center.Only the hindered aminofluorene (IVd) affords a 1:1 mixture of epimers in lower yield. -(FRAY, M.