74476-71-4Relevant academic research and scientific papers
Amide compound and application thereof as TGR5 agonist
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Paragraph 0195-0197, (2017/04/20)
Belonging to the technical field of medicine, the invention in particular relates to an amide TGR5 agonist compound shown as formula (I), its pharmaceutically acceptable salts, esters, stereoisomers, solvent compounds or prodrugs, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X, Y, Z, and ring A are defined as the specification. The invention also relates to a preparation method of the compounds, pharmaceutical preparations, pharmaceutical compositions, and application of the compounds in preparation of drugs for treatment and/or prevention of TGR5 activity regulation related diseases. (formula (I)).
SYNTHESIS OF ETHYL ortho-SUBSTITUTED BENZOYLACETATES AND INVESTIGATION OF THE INFLUENCE OF ortho-SUBSTITUENTS ON KETO-ENOL TAUTOMERISM AND MS FRAGMENTATION BEHAVIOUR
Sicker, Dieter,Mann, Gerhard
, p. 839 - 850 (2007/10/02)
A series of seven ethyl 2-acetyl-(2-substituted benzoyl)acetates II-VIII was synthesized, together with their parent compound I, from the corresponding acid chlorides.The tautomerism of these β-tricarbonyl compounds in tetrachloromethane was studied by 1H NMR spectroscopy and former results concerning this problem were critically evaluated.A further series of seven ortho-substituted ethyl benzoylacetates X-XV and XVII was obtained from the corresponding precursors II-VIII.The keto-enol tautomerism of these β-keto esters was studied by 1H NMR in different solventsand compared with ethyl benzoylacetate IX as standard.Differences caused by the ortho-substituents are discussed.Investigation of the mass spectrometric fragmentation of the β-keto esters IX-XV and XVII showed both common fragmentation pathways due to the same substance class and typical differences in relative intensities according to the nature of the ortho-substituent.
