NEW MATERIAL:An aminomethylphosphonic acid derivative of formulaI(R is lower alkyl other than groups characteristic in the aminoacids constituting protein, phenyl, heterocyclic ring).
EXAMPLE: 2-Thienylalanylaminomethylphosphonic acid.
USE: Antibiotic showing strong effect against gram-positive and -negative bacteria of various kinds. The combination thereof with another antibiotic develops pharamacologically synergic effect.
PREPARATION: A protected aminoacid of formula II (R' is H, lower alkyl; A is amino-protecting group) or its reactive derivative and aminomethylphosphonic acid of formula III or its ester are subjected to condensation reaction to produce an amide of formula IV. Then, the product is deprotected, when necessary, the part of the phosphoric ester is hydrolyzed to give the compound of formulaI.
HIIRAGI MINEJI
WAKIZAKA KIKUO
SUGI HIDEO
TANIGAWA KEIZOU
SUZUKI YUKIO
YAMABE SHIGERU
