Comparison of the stepwise and convergent approaches in the solid-phase synthesis of rat Tyr0-atriopeptin II

Tyr⁰-Atriopeptin II was synthesized on a 2-chlorotrityl resin by both the stepwise and the convergent approach. For both methods an Fmoc/tBu(Trt)-based protection scheme was used. The convergent methodology utilizes the sequential condensation of four protected peptide fragments. These were chosen so that after every condensation reaction, the amino-terminal region of the newly formed resin-bound peptide did not contain a -turn. This designed convergent synthesis gave the target peptide in much higher yield and purity than the conventional step-by-step synthesis.