Abstract
AbstractThe influence of Li‐salts on the course of peptide‐coupling reactions was investigated. As a model for segment couplings, Ac‐Phe‐OH was coupled to HCl·H‐Ala‐OMe using the mixed anhydride, DCC1, DCCl/HOBt, BOP‐Castro and TBTU‐Knorr methods. As a model for stepwise synthesis Z‐Phe‐OH was coupled with HCl·Ala‐O(t‐Bu), using symmetrical anhydrides and active esters. The effects of salt additives such as LiCl, LiBr, LiC104, and ZnCl2 on yields, side‐product formation, racemisation, and reaction rates are reported.
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