METHOD OF L-CARNOSINE AND ITS HOMOLOGS SYNTHESIS Russian patent published in 1997 - IPC

FIELD: medicinal chemistry, biochemistry. SUBSTANCE: invention relates to the improved method of synthesis of L-carnosine and its homologs of the general formula: NH₂(CH₂)_n-CO-His where n = 2-5. Reagent 1: derivative of T-protected amino acid of the formula (I). Reagent 2: L-histidine methyl ether hydrochloride. Process is carried out in aprotonic organic solvent. The synthesized L-carnosine methyl ether derivative protected with N-trityl-group is washed with an alkaline aqueous solution at pH = 7.5-11, extracted with an acid aqueous solution at pH = 0.5-3 and deblocked. Yield is 82-97%. Product exhibits the high purity degree and shows value LD₅₀ = 10000-12000 mg/kg. EFFECT: improved method of synthesis. 1 tbl