Ej. Stoner et al., Synthesis of ABT-378, an HIV protease inhibitor candidate: Avoiding the use of carbodiimides in a difficult peptide coupling, ORG PROC R, 3(2), 1999, pp. 145-148
An alternative to carbodiimide-mediated peptide coupling protocols has been
developed for a carboxylic acid prone to decomposition by polymerization.
This method, involving the in situ generation of an acyl, imidazolide, has
been applied to the preparation of a lead clinical HIV protease inhibitor c
andidate, ABT-378. The nature of the polymerization and optimization of the
new reaction conditions are presented.