Patent ID: 6897289
Filing Date: 2005-05-24
Classification: C07K,Y02P

Abstract:
1. A procedure for solid phase peptide synthesis (SPPS), following a linear or covergent strategy, wherein the peptides contain the sequence of general formula (I): where 30>n>1 wherein 30>n>1; Y=H—, (C X=—OH, —NHCH A as well as all pharmaceutically acceptable salts, for the peptide, formed by addition of acids or complexes thereto, which procedure comprises: a) the use of amino acids with the Nα group protected, through the use of temporary protector groups labile to treatment with basic solutions; b) protecting the side chains of those amino acids which have the chain alkylated or acylated in the final product, with labile protectors stable to acid solutions of type 1 and 2, wherein type 1 solutions are selected from solutions of acetic acid in proportions ranging from 1 to 30% in a solvent, solutions of hexafluoroisopropanol in a solvent different from that used in forming the acetic acid solutions, and equivalent acid solutions, and type 2 solutions are selected from solutions of acetic acid in proportions greater than 30% in a solvent different than that used in the type 1 solutions, solutions of trifluoroacetic acid in proportions lower than 5% in solvents different than those used to form the type 2 acetic acid solutions, and equivalent acid solutions; c) protecting the side chains of at least one of the amino acids that has the chain in free form in the final product, with hyperlabile protectors which are stable to treatment with acid solutions of type 1 and labile to treatment with acid solutions of type 2 indicated above; and d) using a polymeric support that provides peptide-resin bonds which are labile to treatment with acid solutions of type 1 or type 2 indicated above.