2213-09-4Relevant academic research and scientific papers
BIARYL DERIVATIVES AS GPR120 AGONISTS
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Paragraph 730; 739; 740; 741, (2015/01/16)
The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.
Total synthesis of (±)-leporin A
Snider, Barry B.,Lu, Qing
, p. 2839 - 2844 (2007/10/03)
An efficient synthesis of (±)-leporin A (1) has been developed using a tandem Knoevenagel condensation-inverse electron demand intramolecular hetero Diels-Alder reaction to construct the key tricyclic intermediate 3 from pyridone 5 and dienal 6 in one pot in 35% yield. Hydroxylation (71%) of 3 and methylation (77%) of the resulting hydroxypyridone 2 completed the first total synthesis of (±)-leporin A (1).
Preparation of 2-(3-Bromo-1-methylpropyl)-1,3-dioxolan and the Corresponding Chloride from 2-Methylbutyrolactone
Collins, David J.,James, Alison M.
, p. 223 - 228 (2007/10/02)
Lithium aluminium hydride reduction of ethyl 4-chloro-2-methylbutanoate (4a), derived from 3-methyldihydrofuran-2(3H)-one (2-methylbutyrolactone) (1), gave 4-chloro-2-methylbutan-1-ol (5a), oxidation of which with pyridinium chlorochromate afforded 4-chloro-2-methylbutanal (8a).The aldehyde (8a) was converted into 2-(3'-chloro-1'-methylpropyl)-1,3-dioxolan (7a) in 47percent overall yield from (1). 2-(3'-Bromo-1'-methylpropyl)-1,3-dioxolan (7b) was similarly obtained in 49percent overall yield from (1).Attempted conversion of 3-methyltetrahydrofuran-2-ol (2) into the corresponding cyclic ethylene acetal gave epimeric mixtures of 2-(3'-methyltetrahydrofuran-2'-yloxy)ethanol (6) and 2,2'-ethylenedioxybis(3-methyltetrahydrofuran) (9).
