THE COMBINATORIAL SYNTHESIS OF CHIRAL PHOSPHINE-LIGANDS

Chemistry is reported that allows for the synthesis and screening of p hosphine ligands by standard combinatorial technology. To demonstrate the method a 63 member library of phosphine containing peptides was sy nthesized. Rhodium was complexed to the phosphine ligands while they w ere attached to the synthesis support. Each member of the library was screened for its ability to catalyze the asymmetric hydrogenation of e namide (3). Some correlation between specific substitutions in the pri mary sequence of the peptide and the highest enantiomeric excesses was observed. Copyright (C) 1996 Elsevier Science Ltd