FIELD: organic chemistry, chemical technology, biochemistry, medicine.
SUBSTANCE: invention relates to a method for preparing dipeptides eliciting biological activity, in particular, anti-tumor activity that provides their applying in medicinal practice. Invention proposes a method for preparing dipeptides by interaction of N-protected amino acid with esterified amino acid derivative with free amino-group in organic solvent medium in the presence of condensing agent and triethylamine. N-acetyl-L-phenylalanine or N-acetyl-4-[di-(2-chloroethyl)amino]-DL-phenylalanine is used as N-substituted amino acid; L-alanine or L-phenylalanine, or L- and DL-valine methyl or ethyl, or benzyl, or tert.-butyl ester are used as esterified derivative of amino acid; isobutylchlorocarbonate is used as a condensing agent. Triethylamine is taken with 20% excess as regards with stoichiometry value. The proposed method provides preparing dipeptides enriched with DL- or DL + LD-diasteteromers that, therefore, promotes to expanding assortment of preparing peptides used both in scientific-research aims and medicinal practice.
EFFECT: improved preparing method.
1 tbl, 2 ex
Title | Year | Author | Number |
---|---|---|---|
FODDER ADDITIVES REPRESENTED BY DIPEPTIDES | 2010 |
|
RU2536467C2 |
PROCESS FOR PREPARING TRITERPENIC GLYCOPEPTIDES | 1994 |
|
RU2083587C1 |
METHOD OF SYNTHESIS OF N-CARBOXYANHYDRIDES OR URETHANE-PROTECTED N-THIOCARBOXYANHYDRIDES | 1989 |
|
RU2007396C1 |
DERIVATIVES OF HYDRAZINE OR THEIR SALTS, PHARMACEUTICAL AGENT, AMINOALKYLHYDRAZINES OR THEIR SALTS | 1992 |
|
RU2092492C1 |
4-BIMETHYLAMINOPYRIDINE SALTS OF N-PROTECTED AMINO ACIDS AS INTERMEDIATE AGENTS FOR PEPTIDE SYNTHESIS | 0 |
|
SU1253975A1 |
METHOD OF L-CARNOSINE AND ITS HOMOLOGS SYNTHESIS | 1992 |
|
RU2084457C1 |
DERIVATIVES OF 5-AMINO-4-HYDROXYHEXANOIC ACID AND A METHOD OF THEIR SYNTHESIS | 1992 |
|
RU2067585C1 |
DERIVATIVES OF N-ACYLPROLYLDIPEPTIDES | 1993 |
|
RU2119496C1 |
METHOD OF OBTAINING OPTICALLY ACTIVE ALPHA-AMINOACETALES | 2009 |
|
RU2507194C2 |
METHOD OF PREPARING CARBOXY-PROTECTED GLYCOPEPTIDES OF GLYCYRRHIZIC ACID | 1992 |
|
RU2057139C1 |
Authors
Dates
2004-07-27—Published
2002-11-04—Filed