PHOSPHONIC ACID DERIVATIVE

• Format: Patent
• Language: English
• Published: 02.02.1981
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

NEW MATERIAL:A phosphonic acid derivative of formula I (R is thienyl or substituted phenyl). EXAMPLE:1-(beta-2-Thienylalanyl)aminoethylphosphonic acid. USE:Antibacterial agent effective to gram-positive and gram-negative bacteria. PROCESS:The compound of formula I is prepared, e.g. by (1) condensing a protected amino acid of formula II (A is protecting group) or its reactive detivative with an ester of aminoethylphosphonic acid of formula III, in, e.g. a mixed solvent of dimethylformamide and dichloromethane, in the presence of a condensing agent such as dicyclohexylcarbodiimide, and (2) removing the protecting groups and at the same time hydrolyzing the reaction product.