| 摘要 |
<p>An 11 alpha-chlor-6-dimethyl-6-deoxy-6-methylene-5-hydroxy-tetracycline of formula:- (where X is H, Cl or Br) is reacted with an acid R-OH (where R is an organic acid radical with 1 - 10 C atoms) in the presence of one of the reagents methanesulphonic, ethanesulphonic and hydrofluoric acid, or an 11 alpha-chlor-5-hydroxy-tetracycline-6,12-hemiketal of formula: is reacted with a mixture of an organic acid with about 1 - 10C atoms and an alkylsulphonic acid and the compound formed, esterified in the 5-position, is reduced with a reagent to give the free base. Alternatively the acid addition salt is obtained by reaction with a non-toxic acid suitable for pharmaceutical application. The new compounds include the formuloxy, acetyloxy, propioyloxy and butyryloxy methylene tetracyclines.</p> |
