| 摘要 |
The invention comprises o-[2-(acyloxy or hydroxy) acylamino]-phenyl aryl ketones, especially of formula <FORM:1021382/C2/1> wherein ring A may be substituted by 1 or 2 Cl or Br atoms, NO2, C1- 6-alkyl (optionally halogenated) or alkylsulphonyl groups, R, R1 and R2 are H, alkyl, aryl or aralkyl, Ar is aryl and R3 is acyloxy or hydroxy. The acyloxy group may be derived from a carboxylic or a sulphonic acid. Such compounds are prepared by reacting an o-aminophenyl aryl ketone with the appropriate acyloxyacyl halide, anhydride or acid, followed by hydrolysis of the acyloxy to the hydroxy group, if desired. Alternative routes are (a) where the acyloxy group is carboxylic, reacting an o-(2-iodoacetamido)-phenyl aryl ketone with an alkali metal carboxylate; (b) where the acyloxy group is sulphonic, obtaining the corresponding carboxylic acyloxy compound by the general method, hydrolysing off the acyl group and reacting the hydroxy-acylamino compound so obtained with a sulphonyl halide, anhydride or acid. In specified compounds, 2-acetamido-5-chlorobenzophenone is substituted on the side-chain (C) by acetoxy, hydroxy, p-bromophenylsulphonoxy, p-toluene-sulphonoxy, methylsulphonoxy or phenylsulphonoxy. |
