Batchwise peptide synthesis

Batch instruments are generally compatible with both Fmoc//Bu and Bck/ Bzl methods as well as polystyrene, polyethylene glycol-polystyrene graft (PEG-PS). and polyethylene oxide-polystyrene (PEO-PS) supports (for recent reviews see refs 31 and 32). For amino acid activation, protocols have been developed to include carbodiimide, aminium and phosphonium salts, and active esters (pcntafluorophenyl esters and acid halides). For batch instruments designed to monitor the Fmoc function, UV or conductivity detectors are used. 

1 PE Biosystems Model 433A peptide synthesis system 

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In the so-called tea-bag method, originated in 1984 by Houghten et al. [14] for multiple peptide synthesis, the split-pool protocol occurs batchwise on 15 x 22 mm polypropylene mesh packets with pm-sized pores known as tea bags, sealed with resin beads for solid-phase synthesis. This method offers the advantage that a greater quantity of each compound of the library is available at once (up to 500 pmol), which is sufficient for a complete biological and structural characterization. Furthermore, the structural identity of... 

Batchwise solid-phase synthesis, the original procedure of SPPS developed by Mer-rifield in 1966. Alternatively, SPPS can also be performed in a continuous-flow mode solid-phase peptide synthesis using resin-flUed columns. 

For batchwise synthesis, the base matrix used is almost invariably 1% divinylbenzene cross-linked polystyrene (PS). It is relatively inexpensive to produce, swells in the solvents most commonly used in peptide synthesis, namely DCM, DMF, and NMP, and can be readily functionalized using the Friedel-Crafts reaction with chloromethyl, aminomethyl, and benzhydrylamino groups. 

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