- Preparation method of benzoheterocyclic boric acid
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The invention provides a preparation method of benzoheterocyclic boric acid. The preparation method comprises steps as follows: (1) a benzoheterocyclic compound shown in a formula I is dissolved in asolvent A, a liquor A is obtained, a boronylation reagent is dissolved in a solvent B, a liquor B is obtained, a palladium catalyst and an alkaline reagent are immobilized on a channel of a continuousflow reactor, the liquor A and the liquor B are subjected to a continuous adding reaction, the reaction is stopped after the mixture flows out of a reaction tube, and an intermediate is obtained; (2)the intermediate obtained in step (1) is subjected to a hydrolysis reaction, and benzoheterocyclic boric acid is obtained. According to the provided preparation method, the benzoheterocyclic boric acid is synthesized with a flow chemical technology. Compared with methods in the prior art, the method has the advantages that the product yield is 86% or above, the highest yield can reach 90% or above, the yield is very high, the reaction rate is high, energy consumption of a reaction is reduced greatly, and the method is high in operability, high in automation degree and favorable for productionoperation and industrial production.
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Paragraph 0056; 0058; 0060
(2018/09/13)
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- SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
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The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 93
(2015/01/07)
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- Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors
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Figure Presented. Members of a series of 2,4,5-substituted pyrimidine derivatives were synthesized, and their interactions with tubulin and their antiproliferative activities against the human hepatocellular carcinoma cells of liver (BEL-7402) were evaluated. One member of this family, the indole-pyrimidine 4k, having an indole-aryl-substituted aminopyrimidine structure, was observed to be an excellent inhibitor of tubulin polymerization (IC50 = 0.79 μM) and to display significantly high antiproliferative activities against several cancer cell lines with IC 50 values ranging from 16 to 62 nM. This substance displayed a high propensity to arrests cells at the G2/M phase of the cell cycle (EC50 = 20 nM). In addition, 4k was found to competitively inhibit colchicine binding to tubulin, indicating that it binds to the colchicine-binding site of tubulin. The observations made in this investigation demonstrate that 2,4,5-substituted pyrimidines represent a new class of tubulin polymerization inhibitors with significant antiproliferative activity.
- Xie, Fuchun,Zhao, Hongbing,Li, Dewen,Chen, Hong,Quan, Haitian,Shi, Xiaojing,Lou, Liguang,Hu, Youhong
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supporting information; experimental part
p. 3200 - 3205
(2011/07/09)
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