DERIVATIVES OF BORON-CONTAINING PEPTIDES Russian patent published in 1994 - IPC

FIELD: biochemistry, medicine. SUBSTANCE: products: derivatives of boron-containing peptides. Formula is given. Reagent 1: corresponding amine. Reagent 2: R-Z-OH. Condensation is carried out in the solvent in the presence of triethylamine. Product prepared is treated with alkaline metal azide following by reduction in the presence of organic or mineral acid, preferably with benzenesulfoacid, and interaction with cyanamide in lower alcohol at 50-150 C. Formula: , where R₁ - H, Ac, Br, Boc, Boc-Leu; R₂=(CH₂)_nNHC(NH)NH₂; n = 3,4; Y - a residue of pinacone or pinanediol ester; HW - C₆H₅SO₃, HCl, HBr; Z - D- or L-Phe, D-Phe-Pro, D-Phe-Phe, Ala-His, Pro-Phe, Ala-Phe, Thr-Phe, Ala-Glu, Glu-Gly, Gly-Leu-Ala, Pyro-Glu-Phe, Val-Val, D-Val-Leu, Lys-Pro, Leu-Thr. EFFECT: improved method of synthesis. 18 tbl