ALPHA-AMINO ACID DERIVATIVE

• Main Authors: ISHIDA MICHIKO, KASE TOMOKO, SHINOZAKI ATSUHIKO, MIYAKE MASAHISA, TAKAHASHI TOSHIHIRO, TAKEDA HIROMITSU
• Format: Patent
• Language: English
• Published: 30.09.1992
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; 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; HETEROCYCLIC COMPOUNDS; 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

PURPOSE:To obtain a new compound, an antagonist of inhibitory glycine receptor, useful as a treating agent for non-keto-cis type, an agent for central excitatory state, a medicine similar to strychnine and a physical and chemical reagent. CONSTITUTION:A compound shown by formula I (X is sulfo, 1H-tetrazol-5-yl, etc.; R1 to R3 are H, 1-6C alkyl, aralkyl or aryl; R4 to R7 are H, halogen, 1-6C lower or 1-6C lower alkoxy; m and n are 1-8), such as 2-amino-3-[2-(2- phosphonomethyl)phenyl]propionic acid. The compound shown by formula I is obtained by hydrolyzing and decarboxylating a compound shown by formula II (Y1 is 1H-tetrazol-5-yl, etc.; Z is amino-protecting group) under an acidic condition with hydrochloric acid, etc., in a solvent such as acetic acid at 50-120 deg.C for 12-120 hours.