- Sustainable methine sources for the synthesis of heterocycles under metal- and peroxide-free conditions
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Alcohols and ethers were identified as sustainable methine sources for synthesizing quinazolinone and benzimidazole derivatives using a combination of TsOH·H2O/O2 and appropriate bis-nucleophiles for the first time. Deuterium labeling studies clearly proved that the C2 hydrogen of the synthesized heterocycles came from the methine source. These unique reaction conditions were successfully applied to the synthesis of echinozolinone (2e′), 2f′ (a common precursor of rutaecarpine and (±) evodiamine), and dimedazole (6d). Notable features of this method include its low toxicity, use of commercial feedstocks as substrates, low cost, broad functional group tolerance and suitability for a wide range of bis-nucleophilic starting materials.
- Senadi, Gopal Chandru,Kudale, Vishal Suresh,Wang, Jeh-Jeng
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supporting information
p. 979 - 985
(2019/03/12)
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- Efficient syntheses of 2,3-disubstituted natural quinazolinones via iridium catalysis
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Natural products sclerotigenin, pegamine, deoxyvasicinone, mackinazolinone, and rutaecarpine were synthesized. Core quinazolinone structures were constructed via Ir catalysis. The Royal Society of Chemistry 2012.
- Fang, Jie,Zhou, Jianguang
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supporting information; experimental part
p. 2389 - 2391
(2012/04/11)
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- FIBRATE COMPOUNDS HAVING PPAR AGONIST ACTIVITY
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There are provided derivatives having PPAR agonist activity. The derivatives include compounds and/or their pharmaceutically acceptable salts; the compounds having the formula (I) wherein A has the structure (II) or (III); X is chosen from -CH2-, -O-, -NH-, and -S-; Y is chosen from -O-, -NH-, and -S-; Z, which may be located in any position of substitution, is hydrogen or halogen; R1 and R2, which may be the same or different, are independently chosen from hydrogen and C1-C8 alkyl, or R1 and R2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R3 is chosen from hydrogen and C1-C8 alkyl; R4, R5, and R6, which may be the same or different, are independently chosen from hydrogen and C1-C8 alkyl; and n is 1 to 6. Various embodiments and variants are provided. In accordance with other aspects, the invention also provides methods of producing a PPARα agonist activity in a mammal, the methods including administering to the mammal an effective amount of certain derivative(s) of the first aspect of the invention, a method of producing a PPARα agonist activity and a PPARα agonist activity in a mammal, the method including administering to the mammal an effective amount of certain derivative(s); and a pharmaceutical composition that includes the derivative(s) of the first aspect of the invention and one or more pharmaceutically-acceptable excipients. Various embodiments and variants are provided.
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Page/Page column 29
(2010/10/20)
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- Triazolo and derivatives as chemokine inhibitors
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Novel triazolo derivatives represented by the following formula and pharmaceutically acceptable salts thereof, as well as chemokine inhibitors containing the same as an effective component. These are useful as therapeutic agents for allergic diseases such
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