189628-37-3Relevant articles and documents
Monodentate Transient Directing Group Enabled Pd-Catalyzed Ortho-C-H Methoxylation and Chlorination of Benzaldehydes
Li, Feng,Zhou, Yirong,Yang, Heng,Wang, Ziqi,Yu, Qinqin,Zhang, Fang-Lin
supporting information, p. 3692 - 3695 (2019/05/24)
We report Pd-catalyzed ortho-C-H methoxylation and chlorination of benzaldehydes by employing monodentate transient directing groups (TDGs) as an alternative strategy to bidentate TDGs. More importantly, a single crystal of benzaldehyde imine ortho-cyclopalladium intermediate was successfully obtained, and its structure was unambiguously determined by X-ray diffraction, which clearly showed that it was a binuclear palladium species bridged by a pyridone ligand. The utility of this approach was further demonstrated through the synthesis of key intermediates of natural products and drugs.
Preparation method of empagliflozin
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Paragraph 0017, (2018/03/26)
The invention relates to a preparation method of empagliflozin. The preparation method of empagliflozin comprises the following steps: taking 2-chlorobenzaldehyde as a starting material; carrying outbromination reaction, reduction reaction and halogenating reaction on the starting material, and carrying out Friedel-Crafts alkylation reaction on the starting material and (S)-3-phenoxyl tetrahydrofuran to obtain an intermediate which is (S)-3-(4-(5-bromo-2-chlorobenzyl) phenoxyl) tetrahydrofuran; and then carrying out condensation, etherification and methoxyl removal on the intermediate and 2,3,4,6-quadri-O-trimethylsilyl-D-glucolactone to obtain the empagliflozin as a hypoglycemic drug. The preparation method of the empagliflozin has the advantages that compared with an existing synthesisprocess, the preparation method of the empagliflozin takes the 2-chlorobenzaldehyde as the starting material, raw materials are cheap and easy to obtain, industrialization is easy to implement in theprocess, the synthesis route is short, and the method is easy to operate; in a preparation process, various temperature conditions are easy to control, reaction conversion rate is high, and the totalyield can be 75% or above; and moreover, by the preparation method, the product cannot be isomerized easily, impurities are fewer, the purity of the product can be improved, and the purity can be 99%or above.
C-triaryl glucoside compound, preparation method and application of C-triaryl glucoside compound
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Paragraph 0068; 0072-0073, (2018/04/01)
The invention discloses a C-triaryl glucoside compound with the structure shown in the formula I as shown in the description, or an optical isomer thereof, or pharmaceutically acceptable salt, co-crystallization composite, hydrate, solvate or prodrug molecule thereof. The compound disclosed by the invention has a very good selective inhibition effect on SGLT-2, has an obvious promotion effect on releasing of animal urine sugar, can effectively reduce blood glucose and meanwhile cannot result in the risks of weight increase, hypoglycemia and the like. The compound disclosed by the invention haslittle influence on the activity of SGLT-1 while effectively inhibiting the activity of SGLT-2, can be expected that the toxicity is low when being developed into drugs, and has obvious medication advantage.