- Formoterol important intermediate and synthesis method thereof
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The invention discloses a formoterol important intermediate and a synthesis method thereof. 2-bromo-4'-hydroxyacetophenone is used as a raw material. The synthesis method comprises the following steps: dissolving the raw material in concentrated sulfuric acid, adding nitric acid to obtain an intermediate I, dissolving the intermediate I in dichloromethane, adding tert-butyl dimethyl chlorosilane and triethylamine to obtain an intermediate II, dissolving the intermediate II in anhydrous tetrahydrofuran, adding (R)-2-methyl-CBS-oxazboroline and borane-tetrahydrofuran to obtain a chiral intermediate III, dissolving the intermediate III in anhydrous 1,4-dioxane, and adding sodium methoxide to obtain the final product. The synthesis method has the advantages of low cost, simple operation process, low synthesis difficulty and high product yield.
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Paragraph 0014
(2020/05/01)
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- Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists
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Most of reported steroidal FXR antagonists are restricted due to low potency. We described the design and synthesis of novel nonsteroidal scaffold SIPI-7623 derivatives as FXR antagonists. The most potent compound A-11 (IC50 = 7.8 ± 1.1 μM) showed better activity compared to SIPI-7623 (IC50 = 40.8 ± 1.7 μM) and guggulsterone (IC50 = 45.9 ± 1.1 μM). Docking of A-11 in FXR’s ligand-binding domain was also studied.
- Nian, Si-Yun,Wang, Guo-Ping,Jiang, Zheng-Li,Xiao, Ying,Huang, Mo-Han,Zhou, Yi-Huan,Tan, Xiang-Duan
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- Electrophilic tetraalkylammonium nitrate nitration. II. Improved anhydrous aromatic and heteroaromatic mononitration with tetramethylammonium nitrate and triflic anhydride, including selected microwave examples
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A new one-pot nitration employing tetramethylammonium nitrate and trifluoromethanesulfonic anhydride in dichloromethane to provide a ready source of the nitronium triflate nitrating agent is presented. Rapid and selective nitration with a variety of aromatic and heteroaromatic substrates is achieved resulting in the synthesis of several novel organic compounds. A distinct advantage is the removal of undesired byproducts by aqueous workup. This very mild nitration permits large-scale syntheses and gives high isolated product yields that often require no further purification. This tetramethylammonium nitrate-based nitration also has been applied to microwave-assisted conditions, and the results with several compounds are outlined.
- Shackelford, Scott A.,Anderson, Mark B.,Christie, Lance C.,Goetzen, Thomas,Guzman, Mark C.,Hananel, Martha A.,Kornreich, Wayne D.,Li, Haitao,Pathak, Ved P.,Rabinovich, Alex K.,Rajapakse, Ranjan J.,Truesdale, Larry K.,Tsank, Stella M.,Vazir, Haresh N.
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p. 267 - 275
(2007/10/03)
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