38336-04-8Relevant articles and documents
A N - benzyl ethanolamine preparation method
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Paragraph 0023-0028, (2019/06/05)
A N - benzyl ethanolamine preparation method, including the use of ethanolamine and benzyl chloride as the raw material, to solid phase alkali as the reaction of the acid and alkaline catalyst, in the 40 - 120 °C under stirring to carry out the condensation reaction, the reaction after the stop of the take methylethanone, the filtrate to carry out rectification under vacuum, collecting the fraction, product N - benzyl ethanolamine. This invention adopts the solid phase alkali to [...] and catalytic, through the solid-liquid two-phase are a temperature and reaction to improve the main the selectivity of the reaction, in order to improve the synthetic yield; compared with original craft, saves the sodium hydroxide solution used for washing with ethyl acetate extraction of complex process a plurality of times; at the same time as solid phase alkali acid and alkaline catalyst with hydrogen chloride the reaction generates sodium chloride, convenient recycling, realizes the zero discharge of waste water; improves the ethanolamine utilization rate of the raw material; the invention is not only simple and convenient operation, production process economic and environmental protection, few by-products, and the synthetic yield has been raised by 25 - 30%, preparation and reducing the cost to 30 - 35%.
Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives
Lv, Kai,Li, Linhu,Wang, Bo,Liu, Mingliang,Wang, Bin,Shen, Weiyi,Guo, Huiyuan,Lu, Yu
, p. 117 - 125 (2017/06/05)
We report herein the design and synthesis of “novel imidazo [1,2-a]pyridine-3-carboxamides (IPAs)” bearing a variety of different linkers, based on the structure of IMB-1402 discovered in our lab. Results reveal that 2,6-dimethyl-N-[2-(phenylamino)ethyl] IPAs with an electron-donating group on the benzene ring as a potent scaffold. Compounds 26g and 26h have considerable activity (MIC: 0.041–2.64 μM) against drug-sensitive/resistant MTB strains, and they have acceptable safety indices against MTB H37Rv with the SI values of 4395 and 1405, respectively. Moreover, N-[2-(piperazin-1-yl)ethyl] moiety was also identified as a potentially alternative linker (compound 31), opening a new direction for further SAR studies.
Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides
Wang, Minghua,Ye, Cheng,Liu, Mingliang,Wu, Zhaoyang,Li, Linhu,Wang, Chunlan,Liu, Xiujun,Guo, Huiyuan
, p. 2782 - 2787 (2015/06/08)
We report herein the design and synthesis of a series of novel 5-halogenated-7-azaindolin-2-one derivatives containing a 2,4-dimethylpyrrole moiety. Nine target compounds with ≥70% inhibition against MCF-7 at 30 μM were further evaluated for their in vitro antitumor activity against seven human cancer cell lines by SRB assay. Results reveal that some compounds have potent antitumor activity, and the most active 13c7 (IC50s: 4.49-15.39 μM) was found to be more active than Sunitinib (IC50s: 4.70->30 μM) against all of the tested cancer cell lines.