Process for the preparation of peptides

1. A process for the preparation of a compound containing one or more amide bonds using an excess of activated carboxylic component to acylate an amino component, wherein after completion of the acylation reaction an amine comprising a latent anion is added as a scavenger of the residual activated carboxylic functions, which latent anion bears a temporary protecting group which can be selectively removed, followed by a deprotection step resulting in hydrophilic scavenged compounds which may be actively extracted into a basic aqueous phase.

2. The process of claim 1 wherein the temporary protecting group is selectively removed in the presence of a permanent protecting group.

3. The process of claim 1 wherein the compound being prepared is a peptide.

4. The process of claim 2 where the permanent protecting group is attached to the compound.

5. The process of claim 1 wherein the latent anion in the scavenging amine bears a temporary protecting group which displays a lability similar to that of the temporary protecting group present at the N-terminus of the growing compound.

6. The process of claim 1 herein the temporary protecting group is a hydrogenolytically removable groups.

7. The process of claim 2 wherein the permanent protecting group is an acidolytically removable group.

8. The process of claim 6 wherein the temporary protecting group is of the benzyl type.

9. The process of claim 1 wherein the scavenger is a primary amine.

10. The process of claim 9 wherein the primary amine is a C-terminally protected amino acid derivative.

11. The process of claim 10 wherein the amino acid is β-alanine or a derivative thereof.

12. The process of claim 1 wherein the scavenger is a benzyl β-alaninate or a salt thereof.

13. The process of claim 1 comprising performing the process in solution.

14. The process of claim 1 further comprising an aqueous extraction step.