Direct synthesis of Fmoc-protected amines and amino acids using Fmoc-protected iminium ions

ORGN 143

Timothy J. Peelen, peelen@lvc.edu, Alison E. Hartman, aeh002@lvc.edu, Cheryl L. Brophy, clb003@lvc.edu, Julia A. Cupp, Daniel K. Hodge, Kenneth F. Potter II, and Adam D. Wier. Department of Chemistry, Lebanon Valley College, 101 N. College Ave., Annville, PA 17003
The development of solid phase peptide synthesis has created a large demand for Fmoc-protected amino acids. Due the base lability of the Fmoc group, current syntheses of Fmoc-protected amino acids typically require multiple protecting group manipulations. Our goal is to explore more efficient syntheses of Fmoc-protected α- and β-amino acids using Fmoc-protected iminium ions as electrophiles. Toward this goal, we have prepared Fmoc-protected N,O-acetals as bench-stable reagents through simple condensation reactions. In the presence of Lewis acids, the N,O-acetals generate acyliminium ions, which react with weakly basic nucleophiles in a variety of C-C bond-forming reactions. We will describe applications of this chemistry to the syntheses of α- and β-amino acids.
 

Physical Organic Chemistry, Combinatorial and Process Chemistry, New Reactions and Methodology, Peptides, Proteins and Amino Acids
8:00 PM-10:00 PM, Sunday, April 6, 2008 Morial Convention Center -- Hall A, Poster

Sci-Mix
8:00 PM-10:00 PM, Monday, April 7, 2008 Morial Convention Center -- Hall A, Sci-Mix

Division of Organic Chemistry

The 235th ACS National Meeting, New Orleans, LA, April 6-10, 2008