| 摘要 |
<p>NEW MATERIAL:The titled phosphonic acid expressed by formula I (A is mono- to bicyclic heterocyclic ring except 2-thienyl group). EXAMPLE:1-(beta-3-Thienylalanyl)aminoethylphosphonic acid). USE:An antimicrobial agent against vaious bacteria, e.g. Gram-positive and Gram- negative bacteria. PROCESS:A proected substituted alanine (reactive derivative) of formula II (R is a protecting group of the amino group such as carbobenzoxy, t-butoxycarbonyl, formyl, acetyl, etc.) is condensed with a 1-aminoethylphosphonic acid of formula III (R' is H or ester residue consisting of an alkyl groups such as methyl) to form a protected dipeptide intermediate of formula IV. The protecting group of the amino group and the phosphoric acid residue are removed if necessary to give the compound of formula I.</p> |
