- 6-phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiphenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, and in treating hypercholesterolemia
-
6-Phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiophenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, processes for the preparation of these compounds, their use as pharmaceuticals, pharmaceutical preparations and novel phenols and thiophenols Compounds of the general formula I STR1 and the corresponding open-chain dihydroxycarboxylic acids of the formula II STR2 in which X, Y and Z have the meanings given, and pharmacologically tolerated salts thereof with bases and pharmacologically tolerated esters thereof, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. Novel phenols and thiophenols of the formula III STR3 in which X, Y and Z have the meanings given, are also described.
- -
-
-
- Arylation of Phenols. Convenient, Regiospecific Methods for Mono- or Bis-p-fluorophenylations, Suitable for Large Scale Syntheses
-
Phenols have been arylated by a palladium(0)-catalyzed coupling reaction.Two methods were used: a Grignard reagent of a protected phenol component 2 was coupled with a haloarene, or an umpolung (reversed reactivity) where unprotected phenolic halides 6 were coupled with aryl Grignard reagents.Bis-arylation and regiospecific ortho-, meta- and para-arylations were achieved.Aryl-aryl-couplings were insensitive to steric hindrance in the Grignard component, but were inhibited by sulfur-containing substituents in the phenolic component.A thiocyanate substituted biaryl was used to synthesize arylated phenols with various sulfur functionalities.
- Jendralla, Heiner,Chen, Li-Jian
-
p. 827 - 833
(2007/10/02)
-