- Preparation method of 2-methoxy-5-fluorobromoacetophenone
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The invention discloses a preparation method of 2-methoxy-5-fluorobromoacetophenone. The method comprises the following steps: taking p-fluoroanisole as an initial raw material, and reacting with bromoacetyl bromide under the condition of Lewis acid to generate a compound I, namely 2-methoxy-5-fluorobromoacetophenone. In the one-step synthesis route process taking the p-fluoroanisole as the initial raw material, a large amount of reagents with high toxicity and high pollution are avoided, and meanwhile, the raw materials are low in price, so that the whole synthesis process is low in pollution and easy to treat.
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Paragraph 0022-0026; 0027-0029; 0030-0032
(2021/09/08)
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- ROR-GAMMA INHIBITORS
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The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.
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Page/Page column 269
(2019/04/26)
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- Novel hybrids from lamellarin D and combretastatin A 4 as cytotoxic agents
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A new series of hybrids of lamellarin D and combretastatin A 4, 1,2-diphenyl-5,6-dihydropyrrolo [2,1-a] isoquinolines, were designed as cytotoxic agents based on principles of combination in medicinal chemistry and taking the parent compounds' different anti-proliferative mechanisms into consideration. Twenty-two novel hybrids were synthesized through a convenient route, with a key step of core pyrrole formation and evaluated for their anti-proliferative activities in vitro against K-562, A-549, SMMC-7721, SGC-7901 and HCT-116 cancer cell lines. The results showed that some hybrids had good anti-proliferative activities in low IC50 ranges.
- Shen, Li,Yang, Xiaochun,Yang, Bo,He, Qiaojun,Hu, Yongzhou
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body text
p. 11 - 18
(2010/03/03)
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- 3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors
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The C-3 substituents effect on NHE-1 inhibitory activity of (5-arylfuran-2-ylcarbonyl)guanidines, previously identified as potent NHE-1 inhibitors, was investigated. The introduction of amine or alkyl groups at the 3-position of the furan ring, next to the acylguanidine moiety, remarkably improves NHE-1 inhibitory potency. Especially the important finding is that 5-(2,5-dichloro)phenyl and 5-(2-methoxy-5-chloro)phenyl derivatives exhibit high NHE-1 inhibitory activities (IC50 0.02 μM) that match those of 3-unsubstituted derivatives.
- Lee, Sunkyung,Kim, Taemi,Lee, Byung Ho,Yoo, Sung-eun,Lee, Kyunghee,Yi, Kyu Yang
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p. 1291 - 1295
(2008/02/02)
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