Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.

Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.

Disclosed are a series of malonamide derivatives having a chemical structure(I), their synthesis, and evaluation of their bioactivities against bacterial cell, bacterial-infected C.elegans and mice.

Disclosed are a series of malonamide derivatives having a chemical structure(I), their synthesis, and evaluation of their bioactivities against bacterial cell, bacterial-infected C.elegans and mice.

A method for synthesizing 5,8-diamino-3,4-dihydro-2H-1-naphthalenone (Compound I), which method comprises: subjecting 2,5-diprotected aminophenylbutyric acid to the Friedel-Crafts reaction for ring closure, and then removing a protecting group on the amino group to obtain Compound I.

A method for synthesizing 5,8-diamino-3,4-dihydro-2H-1-naphthalenone (Compound I), which method comprises: subjecting 2,5-diprotected aminophenylbutyric acid to the Friedel-Crafts reaction for ring closure, and then removing a protecting group on the amino group to obtain Compound I.

Shown is a compound represented by formula (1). For example, R.sup.1 is alkyl having 1 to 15 carbons; MES is a mesogen group having at least one ring; Sp.sup.1 is a single bond or alkylene having 1 to 10 carbons; M.sup.1 is methyl; and R.sup.2, M.sup.2 and M.sup.3 are hydrogen.

##STR00001##

A compound that is selected from the group consisting of 3-(3,4-dichloroanilino)-3-oxopropanoic acid (hereinafter DCOPA); N-methyl-DCOPA; N,2-dimethyl-DCOPA; 2-methyl-DCOPA; isobutyl-DCOPA; N-methyl-isobutyl DCOPA; 3-(3,4-bibromoanilino)-3-oxopropanoic acid; and analogs of DCOPA; and analogs of 3-(3,4-bibromoanilino)-3-oxopropanoic acid; and pharmaceutically acceptable salts of these compounds, are disclosed. A method of controlling bone erosion in a patient comprising administering to the patient a therapeutically effective amount of at least one of these compounds, or a pharmaceutically acceptable salt of at least one of these compounds, is provided. A method of reducing inflammation in a patient having an inflammatory condition comprising administering to the patient a therapeutically effective amount of at least one of these compounds, or a pharmaceutically acceptable salt of at least one of these compounds is provided.

A compound that is selected from the group consisting of 3-(3,4-dichloroanilino)-3-oxopropanoic acid (hereinafter DCOPA); N-methyl-DCOPA; N,2-dimethyl-DCOPA; 2-methyl-DCOPA; isobutyl-DCOPA; N-methyl-isobutyl DCOPA; 3-(3,4-bibromoanilino)-3-oxopropanoic acid; and analogs of DCOPA; and analogs of 3-(3,4-bibromoanilino)-3-oxopropanoic acid; and pharmaceutically acceptable salts of these compounds, are disclosed. A method of controlling bone erosion in a patient comprising administering to the patient a therapeutically effective amount of at least one of these compounds, or a pharmaceutically acceptable salt of at least one of these compounds, is provided. A method of reducing inflammation in a patient having an inflammatory condition comprising administering to the patient a therapeutically effective amount of at least one of these compounds, or a pharmaceutically acceptable salt of at least one of these compounds is provided.

The present invention relates to a process for preparing substituted biphenylanilides of the formula (I)

##STR00001##

in which R.sup.1 is selected from a protected amino group, NO.sub.2, NH.sub.2 and NHR.sup.3,
in which a compound of the formula II

##STR00002##

is reacted in the presence of a base and of a palladium salt, in the presence of a phosphine ligand of the formula (V) as complex ligand

##STR00003##

or a salt thereof, in a solvent, with an organoboron compound of the formula (III)

##STR00004##

in which all the substituents are as defined in the description.