Peptide synthesis by using polymer‐supported N‐acylphosphoramidites

Diethoxyphosphino-substituted acetamides (1 and 2) and the polymer gel bearing dialkoxy-phosphino groups (3,4, and 5) were prepared by reaction of chlorophosphites with acetamide and crosslinked polyacrylamides, respectively, in the presence of triethylamine. By using 1,2 and the polymer as condensing reagents, various peptides were synthesized directly from N-protected amino acids and amino acid esters in high yields with little racemization. The highly crosslinked polymeric reagents simplified the procedure and were recycled by treatment with chlorophosphites.