| abstract |
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. n CONSTITUTION: A compound shown by formula I (X is sulfo, 1H-tetrazol-5-yl, etc.; R 1 to R 3 are H, 1-6C alkyl, aralkyl or aryl; R 4 to R 7 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 (Y 1 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°C for 12-120 hours. n COPYRIGHT: (C)1992,JPO&Japio |