- Fe-catalyzed regiodivergent [1,2]-shift of α-aryl aldehydes
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An Fe-catalyzed conversion of aldehydes to ketones via [1,2]-shift has been developed. This skeletal rearrangement shows a wide substrate scope and chemoselectivity profile while exhibiting an excellent [1,2]-aryl or [1,2]-alkyl shift selectivity that is easily switched by electronic effects.
- Gutierrez-Bonet, Alvaro,Flores-Gaspar, Areli,Martin, Ruben
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supporting information
p. 12576 - 12579
(2013/09/23)
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- Broonsted acid-promoted hydrocyanation of arylalkenes
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Nonactivated arylalkenes are effectively converted to tertiary benzylic nitriles in the presence of triflic acid and trimethylsilyl cyanide. The hydrocyanation reactions result in good to excellent yield when electron-donating groups are substituted on the benzene ring. The reaction conditions are mild and relatively safe, notably without need for handling hazardous hydrogen cyanide gas, providing simple and easy access to tertiary benzylic nitriles. The reaction was applied to the preparation of a PDE4 inhibitor (3) as well as a series of analogues.
- Yanagisawa, Arata,Nezu, Tetsuya,Mohri, Shin-Ichiro
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supporting information; experimental part
p. 5286 - 5289
(2009/12/29)
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- N-SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISORDERS
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The present invention relates to N-substituted heterocyclic derivatives of formula: STR1 processes for their preparation, and pharmaceutical compositions which contain them. The compounds according to the invention are non-peptide compounds which oppose the action of angiotensin II. The compounds according to the invention are thus useful in the treatment of cardiovascular disorders such as hypertension and heart failure.
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- Novel arylcycloalkanepolyalkylamines
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Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.
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