Representative No: WO/2015/128687
Type of IP: Patent
Industry: Pharmaceutical and cosmetics industry
The invention relates to a continuous flow chemical method for the solid phase synthesis of peptides and enantiomers, diastereomers, stereoisomers, mixtures, salts and/or derivatives thereof. Biopolymers constituting the basis of life, like oligo- and polysaccharides, oligo- and polynucleotides, and oligo- and polypeptides are of considerable interest. Peptides and proteins are polymers built from amino acids. The present invention is based on the unexpected finding that using the continuous flow technology to the solid phase peptide synthesis the amino acid excess can be reduced to a range of 1 to 1.5 equivalents and peptides of high purity can be synthesized with practically complete couplings and in good yields if the synthesis is performed at elevated temperature and pressure. Currently applied technical methodologies require the application of high amino acid excess and the obtained yields are not satisfactory. According to the present invention nearly 100% coupling can be reached also when using low amino acid excess during the peptide synthesis and even in the case of peptides comprising strongly structure promoting amino acids the yields are excellent.