Dipropylamine for 9-Fluorenylmethyloxycarbonyl (Fmoc) Deprotection with Reduced Aspartimide Formation in Solid-Phase Peptide Synthesis

Herein, we report dipropylamine (DPA) as a fluorenylmethylox-ycarbonyl (Fmoc) deprotection reagent to strongly reduce aspartimide formation compared to piperidine (PPR) in high-temperature (60 degrees C) solid-phase peptide synthesis (SPPS). In contrast to PPR, DPA is readily available, inexpensive, low toxicity, and nonstench. DPA also provides good yields in SPPS of non-aspartimide-prone peptides and peptide dendrimers.

Automated summary

Here, we demonstrate that dipropylamine (DPA) can effectively reduce aspartimide formation in high-temperature solid-phase peptide synthesis (SPPS) compared to piperidine (PPR). DPA is easily accessible, inexpensive, non-toxic, and odorless, making it a promising alternative to PPR. Furthermore, DPA yields good results in SPPS of non-aspartimide-prone peptides and peptide dendrimers.