Rapid Solid-Phase Synthesis of a Calmodulin-Binding Nonapeptide using Thermal and Controlled Microwave Irradiation

B. Bacsa, B. Desai, G. Dibó1 and C.O. Kappe, Eötvös Loránd University and Karl-Franzens-University Graz

Recently, there are a growing number of publications that report the use of microwave heating for solid-phase organic synthesis, either by using a variety of polymeric supports or applying polymer-supported reagents and catalysts.

Although solid phase synthesis was originally introduced for the preparation of oligopeptides in 1963 by R.B. Merrifield, surprisingly, there are only a few reports so far on the use of microwave irradiation for the preparation of peptides and related species.

In fact, it is widely accepted that microwave-assisted chemical reactions can be completed in minutes, providing less by-products and higher yields. Moreover, due to the recent progress in microwave technology, a new generation of the microwave ovens reached the market.

By using the latest developments in microwave technology, we developed various protocols for the synthesis and fluorescently labelling of test peptides under microwave conditions. All synthetic steps were performed under very mild conditions, similar to that is used in traditional solid-phase peptide synthesis. After the final cleavage step, the crude peptide product was subjected to HPLC-MS analysis.

As it was expected, the reaction time of each step decreased from hours to minutes, and the peptides were obtained in better yields and higher purity by the MAPS strategy, as compared to peptides synthesized by classical SPPS protocols.

Click here to open PDF

---

Comments about this Poster

Click Here to Leave a Comment about this Poster