915095-85-1Relevant articles and documents
Preparation method of polysubstituted diphenyl ketone
-
Paragraph 0054; 0071-0078; 0085-0087, (2021/09/21)
The preparation method comprises the following steps: (1) a compound represented by the formula II and a compound shown III as a raw material; and synthesizing the compound as shown IV. (2) The compound of Formula IV is subjected to Fries rearrangement to produce a compound of Formula V. (3) A compound of Formula V is subjected to a halogenation reaction in contact with a halogenation reagent to prepare a multi-substituted diphenyl ketone represented by Formula I. Wherein, X is selected from H, F, Cl, Br, I. R1 Selected H from F Cl, Br I are RO selected R from H, C1 - C6. X is selected from F, Cl, Br, and i. The present invention is capable of improving the yield and selectivity of the target product.
A NEW HETEROCYCLIC COMPOUND: CRYSTAL STRUCTURE AND ANTICANCER ACTIVITY AGAINST HUMAN LUNG ADENOCARCINOMA CELLS
Li, H.,Li, X. X.,Shen, L.,Shi, E. H.,Wang, L. R.,Zhang, C. Y.,Zhang, D. L.,Zhao, S.
, p. 1167 - 1174 (2020/09/09)
Abstract: New heterocyclic compound (S)-3-(4-(5-bromo-2-chlorobenzyl)phenoxy)tetrahydrofuran (1), designed by utilizing 5-bromo-2-chlorobenzoic acid (2) as the starting material, is obtained by the organic synthesis and then characterized by single crystal X-ray crystallography, 1H NMR and IR spectroscopy. In the biological study, the CCK-8 assay is performed to evaluate the inhibitory effect of the compound on SPC-A-1 human lung adenocarcinoma cells in vitro by measuring the cancer cell viability. Then, the anticancer activity of the compound is also confirmed by the in vivo xenograft experiment by measuring the mice body weight and the cancer volume.
Synthetic method for preparing empagliflozin intermediate
-
Paragraph 0050; 0051; 0053; 0056; 0058, (2020/07/02)
The invention discloses a synthetic method for preparing an empagliflozin intermediate. The method comprises the following specific steps: 1) mixing a compound I with a solvent, preparing a compound II by using an acylation reagent, adding the compound II into a system of fluorobenzene and aluminum trichloride, carrying out a Friedel-Crafts reaction at room temperature, performing quenching with water, conducting liquid separation and washing successively, and concentrating an organic matter to obtain a compound III; 2) adding the compound III into a reaction kettle, adding a solvent, an alkali and a catalyst, then adding a compound IV, carrying out heating for a reaction, performing washing with water after the reaction, and conducting concentrating and crystallizing to obtain a solid compound V; and 3) adding the compound V into the reaction kettle, adding a solvent, an acid and a reducing agent, carrying out quenching with water after a reaction, conducting liquid separation and washing successively, concentrating an organic matter, and carrying out crystallizing to obtain a solid compound V. The method is simple and safe in process, high in product yield, easy in impurity control and suitable for industrial production.