- 4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters and a process for their preparation
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4-Hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, process for their preparation, their use as pharmaceuticals, and pharmaceutical preparations and precursors. Compounds of the formula I STR1 and the corresponding open-chain dihydroxycarboxylic acids of the formula II STR2 in which X, Y, R1, R2, R3, R4 and R5 have the meanings indicated, and also their pharmacologically tolerable salts with bases and their pharmacologically tolerable esters, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. In addition, compounds of the formula III STR3 in which R1, R2, R3, R4, R5, X and Y have the meanings indicated are described.
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- Arylation of Phenols. Convenient, Regiospecific Methods for Mono- or Bis-p-fluorophenylations, Suitable for Large Scale Syntheses
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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
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p. 827 - 833
(2007/10/02)
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