Phosphine and phosphite gold complexes of thiobenzoic acid and substituted thiophenols and their use

摘要

1422508 Phosphorus-containing gold complexes SMITHKLINE CORP 17 July 1974 [23 July 1973] 31556/74 Heading C2P The invention comprises compounds of the formula wherein RSP1/SP is C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl or phenoxy, Y is -C(O)- or a C-S single bond, RSP2/SP is H, NH 2 or COOM when Y is C=O, or is NH 2 or COOM when Y is a C-S single bond and M is H or an alkali metal cation. The compounds are prepared by reacting an appropriately substituted or unsubstituted thiobenzoic acid or an appropriately substituted thiophenol with an appropriate triorganophosphine or phosphite gold halide, in the presence of alkali, e.g. NaOH or KOH, in a solvent such as ethanol or aqueous ethanol at about 25‹ C. for approximately 1 hour. When RSP2/SP is to be carboxy and RSP2/SP is initially COOM the reaction mixture is acidified to liberate the free acid. The products have anti-arthritic activity and for this purpose may be used as active ingredients in pharmaceutical compositions, especially compositions in dosage unit forms of conventional type. Triphenylphosphite gold (I) chloride is obtained by reacting a mixture of gold acid chloride trihydrate and thiodiglycol in cold aqueous ethanol with a cold solution of triphenyl phosphite in ethanol.