863031-21-4Relevant articles and documents
Polymorphs and solvatomorphs of azilsartan medoxomil: Elucidation of solvent-induced construction and conformational diversity
Zhang, Xian-Rui,He, Sai-Fei,Zhang, Shuo,Li, Jing,Li, Shan,Liu, Jin-Song,Zhang, Lei
, p. 103 - 113 (2017)
Two polymorphs (AM-A and AM-B) of azilsartan medoxomil (AM) and four AM solvatomorphs with toluene (AM-TOL), 1,4-dioxane (AM-DIO), chloroform (AM-TCM) and N,N-dimethylacetamide (AM-DMA) have been prepared by the hydrolysis of azilsartan medoxomil potassium in aqueous-organic solutions. In the crystal structures of two polymorphs and three solvatomorphs (AM-TOL, AM-DIO and AM-TCM), two asymmetric AM molecules form the dimeric cycle-like structures via intermolecular N[sbnd]H?N hydrogen bonds in R22 (26) ring, while AM-DMA shows intramolecular N[sbnd]H?O hydrogen bond between AM and DMA molecules. The hydrogen bonds (C[sbnd]H?O or C[sbnd]H?N) and π···π (or C[sbnd]H···π) interactions are helpful to stabilize the conformational diversity of AM. The solvent-induced experiment shows that solvent molecules have great influence on the solvatomorph formation and DIO can form the most steady solvatomorph than other solvents. The thermal study demonstrates that toluene molecules in three solvatomorphs (AM-TOL, AM-DIO and AM-TCM) are the most difficult to remove from the cage. Our results illustrate that the solvent plays significant role in tuning the size of the cage and producing the conformational diversity of AM molecules.
Preparation method of azilsartan kamedoxomil hydrate
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Paragraph 0061; 0064, (2018/09/08)
The invention provides a preparation method of azilsartan kamedoxomil hydrate. The preparation method at least comprises the following steps: (1) performing the chlorination; (2) performing the esterification; (3) forming azilsartan kamedoxomil; and (4) forming the azilsartan kamedoxomil hydrate. The preparation method has the characteristics of simple operation, high yield, high purity and good stability, and is suitable for industrialized production.
A method for preparing arab League Qi Shatan ester (by machine translation)
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Paragraph 0018 - 0021; 0046 - 0049, (2016/10/08)
The invention relates to a method of synthesizing arab League Qi Shatan ester, the method to the 4 [...] -bromo methyl-2-cyano biphenyl as the raw material and then by the hydroxylamine compound II is prepared by cyclization; to 2-ethoxylbenzimidazole-7-carboxylic acid as raw materials to carry out the esterification reaction to make compound V, then utilize the compound prepared with compound II arab League Qi Shatan ester V reaction. The method of the present invention the synthetic route is short, the operation is simple, high yield, at the same time reduces the raw material 4 the [...] -bromomethyl-2-cyanobiphenyl consumption, the cost is reduced. (by machine translation)