Simple, economical and flexible apparatus for solid phase peptide synthesis

Abstract

Solid phase peptide synthesis basically involves repetitive deblocking and coupling reactions. In order to make these repetitive operations fast and convenient, the deblocking and coupling reactions are carried out in specially designed apparatus, which are called solid phase peptide synthesis apparatus. These apparatus are expensive, hence unaffordable for many laboratories. In addition, these apparatus lack the operational flexibility for varying reaction parameters such as reaction time, temperature, pressure, sonication, microwave irradiation, etc. In order to make peptide synthesis convenient and flexible with respect to reaction conditions and affordable for many laboratories, a two-vessel approach has been proposed. In this approach, coupling reaction is carried out in a round bottom flask with overhead stirrer, and the filtration (work-up) is carried out in a specially designed filtration-vessel. Using the two-vessel approach, D-Met-enkephalins (pentapeptides, Tyr-Gly-Gly-Phe-D-Met) and some of its derivatives involving lengthy reactions have been synthesized on Merrifield resin. This approach is very convenient for studying variations in reaction conditions and is good for synthesizing short peptides (<10 amino acids). By this approach 1-100 g resin can be handled in a laboratory without any additional cost. This approach can be extrapolated to solid phase syntheses as well.