- Decarboxylative Amination: Diazirines as Single and Double Electrophilic Nitrogen Transfer Reagents
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The ubiquity of nitrogen-containing small molecules in medicine necessitates the continued search for improved methods for C-N bond formation. Electrophilic amination often requires a disparate toolkit of reagents whose selection depends on the specific structure and functionality of the substrate to be aminated. Further, many of these reagents are challenging to handle, engage in undesired side reactions, and function only within a narrow scope. Here we report the use of diazirines as practical reagents for the decarboxylative amination of simple and complex redox-active esters. The diaziridines thus produced are readily diversifiable to amines, hydrazines, and nitrogen-containing heterocycles in one step. The reaction has also been applied in fluorous phase synthesis with a perfluorinated diazirine.
- Chandrachud, Preeti P.,Wojtas, Lukasz,Lopchuk, Justin M.
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p. 21743 - 21750
(2021/01/11)
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- ASK1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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The present disclosure relates to a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.
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Paragraph 0492
(2020/01/02)
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- COMPOUNDS AND THERAPEUTIC USES THEREOF
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The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
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Page/Page column 104
(2010/11/03)
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- 2-SUBSTITUED 5, 6-DIARYL-PYRAZINE DERIVATIVES AS CB1 MODULATOR.
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The present invention relates to 5, 6-diaryl-pyrazine-2-carboxamide and- 2-ester derivatives and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. The compounds are cannabinoid receptor 1 (CB1) modulators.
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- GUANIDINO-SUBSTITUTED QUINAZOLINONE COMPOUNDS AS MC4-R AGONISTS
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A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
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Page/Page column 154
(2008/06/13)
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- Substituted quinazolinone compounds
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A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variab
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- SUBSTITUTED QUINAZOLINONE COMPOUNDS
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A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or (IC): where the v
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