Solid support synthesis of 2-oxopiperazines

摘要

The subject invention involves processes for making 2-oxopiperazine and homologous compounds using a solid support resin by (a) removing the protecting group from an N-protected amino acid ester of the resin (if present), (b) reacting the resulting unprotected resin ester with a N-protected alpha -amino aldehyde, (c) optionally modifying the resulting intermediate by substituting a non-hydrogen moiety on the N from the amino acid, (d) removing the remaining N-protecting group from the N from the amino aldehyde, and (e) cleaving/cyclizing the product from the resin.