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    Empagliflozin

    Empagliflozin ??? ???
    ?? ??:
    864070-44-0
    ???:
    Empagliflozin
    ???(??):
    ozin;Empag;CS-798;EmpagL;BI-10773;Glyxambi;Empaglifloin;mpagliflozin;Empagli ozin;EMpagliflozin
    CBNumber:
    CB52627802
    ???:
    C23H27ClO7
    ??? ??:
    450.91
    MOL ??:
    864070-44-0.mol

    Empagliflozin ??

    ?? ?
    665℃
    ??
    1.398
    ???
    356℃
    ?? ??
    Sealed in dry,2-8°C
    ?? ?? (pKa)
    13.23±0.70(Predicted)

    ??

    Empagliflozin C??? ??, ??, ??

    ??

    Empagliflozin (??? Jardiance)? 2014?? ??? ?? ??-2 ???? ??? ?? ???? gliflozin ??? ? ???. ??? Boehringer Ingelheim? ?? Eli Lilly Company ????.

    ??

    Empagliflozin? ??? ??? CO ???? 2 (SGLT-2)? ???, ? ??? ?? ?? ?? ???? ??? ?? ???? ??????????.

    ??

    Empagliflozin, a sodium-glucose co-transporter 2 (SGLT2) inhibitor, was originally discovered by Boehringer Ingelheim and codeveloped and co-marketed through research collaboration with Eli Lilly and Co. It was first approved by European Medicine Agency (EMA) in May 2014, followed by the approval of the US FDA in August 2014. SGLT2 inhibitors are anewclass of glucose-lowering agents developed for the treatment of type 2 diabetes mellitus, which have a mechanism of action that is independent of pancreatic b-cell function or the degree of insulin resistance. Consequently, SGLT2 inhibitors have the potential to be of use not only as standalone therapy but also in combination with any of the existing classes of glucose-lowering agents, including insulin. Empagliflozin selectively inhibits SGLT2, which in turn prevents glucose reabsorption by excreting excess glucose in the urine.

    ??

    Empagliflozin is a novel, potent and selective SGLT-2 inhibitor, improves glycaemic control and features of metabolic syndrome in diabetic rats.

    ??

    ChEBI: A C-glycosyl compound consisting of a beta-glucosyl residue having a (4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl group at the anomeric centre. A sodium-glucose co-transporter 2 inhibitor u ed as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

    Chemical Synthesis

    Commercial 5-iodo-2-chlorobenzoic acid (97) was first converted to the corresponding acid chloride, prior to subjection to commercially available fluorobenzene (98) under Friedel–Crafts conditions to generate the desired fluorobenzophenone 99 in 94% yield after isolation by recrystallization from aqueous isopropanol. The fluorobenzophenone (99) was then reacted with commercially available (S)-3-hydroxytetrahydrofuran (100) and potassium tertbutoxide in THF to afford ethereal benzophenone 101. Next, removal of the ketone functionality within 101 was achieved through the use of 1,1,3,3-tetramethyldisiloxane (TMDS) in the presence of aluminum chloride in toluene to deliver diaryl iodide 102. This iodide was subsequently converted to the corresponding Grignard reagent and subjected to gluconolactone 103, giving rise to an intermediate lactol which was then sequentially treated with aqueous citric acid, methanolic HCl, and triethylsilyl hydride and aluminum trichloride to ultimately furnish empagliflozin (XIII) in 73% yield across the four-step protocol.

    Empagliflozin ?? ?? ? ???

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    Empagliflozin ?? ??

    ???( 445)?? ??
    ??? ?? ?? ??? ?? ?? ? ??
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