| 摘要 |
Peptidyl-amino-alkylphosphonic acids of formula R1NHCH2PO3H2 (Ia) and R2NHCH(Me)PO3H2 (Ib) are new, where: R1 = L-4-fluorophenylalanyl, L-3-nitrotyrosyl, L-4-aminophenylalanyl, L-2,4-dichlorophenylalanyl, L-3,4-dichlorophenylalanyl, L-beta-methyl-phenylalanyl, alpha-methylalanyl, Gly-L-Val, L-Phe-L-Leu, L-Leu-L-Leu, Gly-L-Tyr or L-Ala-sarcosyl; R2 = L-3-nitrotyrosyl, L-Ala-L-Leu, sarcosyl-L-Phe, L-Leu-L-Phe, L-Leu-L-Leu, sarcosyl-L-Leu, L-Leu-L-Ala, L-Ala (L-arginine or 2-amino-2-hydroxymethyl-1,3-propanediol salt), Gly-L-Leu, N-acetylglycyl-L-Leu, sarcosyl-L-Tyr, L-Pro-L-Leu or N-benzylglycyl-L-Leu; the NHCH(Me)PO3H2 gp. is in the L configuration. - Prods. obtd. by contacting (Ib; R2 = L-Ala) with a weakly basic polyamine-phenolic resins, polystyrene sulphonic acid resins and strongly basic polystyrene resins are also new. Prodn. of phosphonic di- or tripeptides (I) with an L configuration is effected by reacting 1 mole of an alpha-amino carboxylic acid or an L-dipeptide formed from two L- or DL-alpha-amino carboxylic acids with at least 2 moles of a DL-alpha-amino phosphonic acid (II) or an L-phosphonic dipeptide formed from (II) and an alpha-amino carboxylic acid. The reaction is effected in an acidic aq. medium at 10-70 deg.C in the presence of papain or chymopapain.
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