The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.

1,2,4-Oxadiazole benzoic acid compounds and their use for nonsense suppression and the treatment of disease

Bronsted acid catalyzed tandem cyclization was found to be highly effective for the preparation of a series of polysubstituted 4-pyrones from diynones (yield up to 99%). 4-Pyridone and 3-pyrrolone derivatives were also selectively synthesized by employing NIS and/or Bronsted acid. NIS as an electrophilic reagent could promote these reactions efficiently and rapidly under very mild reaction conditions.

Brønsted acid catalyzed and NIS-promoted cyclization of diynones: selective synthesis of 4-pyrone, 4-pyridone, and 3-pyrrolone derivatives.

The synthesis of different 3,5-disubstituted isoxazoles and related isoxazolines using choline chloride:urea as deep eutectic solvent (DES) in a one-pot three step reaction has been accomplished successfully. The use of highly nucleophilic functionalized DES did not affect the process where highly electrophilic reagents or intermediates are involved. The presence of DES showed to be essential since the reaction in absence of this media did not proceed. The DES media could be reused up to five times without a detrimental effect on the yield of the reaction. To exemplify the synthetic potential of this methodology, the reaction was scaled up to the gram scale without any noticeable problem. Finally, different isoxazoles were easily transformed into β-aminoenones.

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Synthesis of 3,5-Disubstituted Isoxazoles and Isoxazolines in Deep Eutectic Solvents

A concise approach to 5-substituted-4-pyrones from kojic acid

Catalyst Control in Positional-Selective C-H Alkenylation of Isoxazoles and a Ruthenium-Mediated Assembly of Trisubstituted Pyrroles.

Synthesis of pyran-4-ones from isoxazoles

A synthesis of mono-, di- and tri-substituted pyran-4-ones from isoxazoles is reported. The isoxazoles can be synthesized from readily available starting materials and undergo a reductive cleavage reaction with Mo(CO) 6 to generate enamino ketone intermediates, which are then cyclized to pyran-4-ones under acidic conditions.

Edith Lacasse

Papers

Synthesis of pyran-4-ones from isoxazoles

Synthesis of Pyran-4-ones from Isoxazoles.