METHOD FOR ACCELERATED PEPTIDE SYNTHESIS IN SOLUTION Russian patent published in 2004 - IPC

FIELD: chemistry of peptides, organic synthesis.

SUBSTANCE: invention relates to a method for accelerated peptide synthesis in solution. Method involves repeating cycles of stages (a) - (d): (a) condensation stage using excess of activated carboxyl component that acylates amino-component; (b) quenching stage wherein acceptor is used for removing residual activated carboxylic functions and wherein this acceptor can be used for deblocking a peptide to be spliced also; (c) one or more aqueous extractions and, optionally, (d) separate deblocking stage carrying out after one or more extractions. Method involves at least one stage (b) that is named as stage (b') wherein amine comprising free anion or latent anion representing, respectively, deblocked amino acid or derivative of blocked amino acid is used as acceptor of residual activated carboxylic functions. Using this method the splicing peptide is not isolated as long as the final peptide sequence will be prepared. This highly effective method can be used for preparing oligopeptides and polypeptides with high degree of purity.

EFFECT: improved method for peptide synthesis.

26 cl, 2 ex