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.
NOVEL PROCESSES FOR PREPARATION OF DAPAGLIFLOZIN OR ITS SOLVATES OR CO-CRYSTALS THEREOF
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Page/Page column 60, (2018/03/06)
The present invention generally relates to an improved process for the preparation of dapagliflozin of Formula I or its solvates or co-crystals thereof. The present invention also encompasses the novel intermediates and their use in the preparation of dap
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.