P-SUBSTITUTED PROPANE-PHOSPHINIC ACID COMPOUNDS

摘要

4-17594/+ P-substituted Propane-Phosphinic Acid Compounds Compounds of the formula I (I), wherein either R1 is halogen, R1' is halogen or hydrogen and R2 and R2' denote hydrogen or R1 and R1' represent hydrogen, R2 is an aliphatic or aromatic radical and R2' is hydroxy or R2 and R2' together represent oxo, and wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms or, if R1 and R1' denote hydrogen, R2 represents an aromatic radical and R2' is hydroxy, R represents methyl, and their salts are useful as nootropics, antidepressants and/or anxiolytics. The can be manufacture by replacing any group R5 by hydrogen and/or converting any group Zo into amino in a compound of formula II (II) in which R, R1, R1', R2 and R2' have their previous significances, Z represents a protected or latent amino group Z0 and R4 denotes hydrogen or a hydroxy-protective group R5, and wherein amino as a constituent of R and/or hydroxy R2' or oxo R2 + R2' may be present in a temporarily protected form.