Novel hydroxylated and alkoxylated n- and/or p-aralkyl-phosphinic acid derivatives

摘要

Hydroxylated or alkoxylated N,P-aralkylphosphinic acid derivatives of formula (I) wherein R1 denotes an aliphatic, cycloaliphatic or aromatic group, R2 and R5 independently of each other, represent hydrogen or an aliphatic group, R3 denotes hydrogen or hydroxy and R4 denotes hydrogen or R3 and R4 together represent oxo, R6 denotes hydrogen or [<3>H]- or [<11>C]-labeled alkyl, R7 denotes hydrogen, lower alkyl, lower alkoxy, halogen, carboxy, carbamoyl or cyano, and wherein one of X1 and X2 represents a group of the formula >N- and the other represents a group of the formula >P(=O)(OH)-, and their salts are novel. Compounds of formula (I) wherein R6 denotes hydrogen, can be easily converted into the corresponding compounds of formula (I) in which R6 denotes [<3>H]- or [<11>C]-labeled alkyl, and optionally into pharmaceutically acceptable salts thereof which can be used as a tool for localization and assessment of GABAB receptor sites in the mammal central nervous system by means of ex vivo autoradiography or in vivo Positron Emission Tomography (PET).