Combinatorial synthesis of the peptidomimetic inhibitors of HIV 1 protease

A cobalt-catalyzed combinatorial synthesis of various β-phenylisoserine derivatives is described. This methodology is applied to a one-pot synthesis of pyrrolidine- containing α-hydroxyamide core structure, β-phenylisoserine-valine dipeptide isostere and α-acetyl- or α-hydroxyethyl-β-amino acid derivatives. 1 Roberts N A, Martin J A, Kinchington D, Broadhurst A V, Craig, J C, Duncan I B, Galpin S A, Handa B K, Kay J, Krohn A, Lambert R W, Merrett J H, Mills J S, Parkes K E B, Redshaw S, Ritchie A J, Taylor D L, Thomas G J & Machin P J, Science, 248, 1990, 358.