75227-41-7Relevant academic research and scientific papers
2 - [6-methoxy-3 - (2,3-dichlorophenyl) methyl-4-oxo -1,4-dihydro -1 (4H)-quinolyl] method for the preparation of acetic acid
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, (2016/10/08)
The invention provides a preparation method of 2-(6-methoxy-3-(2, 3-dichlorophenyl) methyl-4-oxo-1, 4-dihydro-1(4H)-quinolyl) acetic acid. The preparation method comprises the following steps: by taking 3-(4-methoxyanilino) sodium propionate as a raw material, performing amino protection treatment to prepare 3-(N-protecting group-4-methoxyanilino) propionic acid, performing Friedel-Crafts acylation reaction to prepare N-protecting group-6-methoxy-2, 3-dihydroquinolinone, and further performing deprotection treatment to prepare an intermediate, namely 6-methoxy-2, 3-dihydro-4 (1H)-quinolinone; by taking the intermediate, namely 6-methoxy-2, 3-dihydro-4 (1H)-quinolinone as a raw material, performing N-alkylation, hydrolysis and condensation reaction to prepare a target product. By adopting the preparation method, the use of a large amount of polyphosphoric acid (PPA) can be avoided, the process is environment-friendly, and the preparation method is more conductive to industrial production.
Structure-activity relationships of antimalarial indoloquinolines
Werbel, L. M.,Kesten, S. J.,Turner, W. R.
, p. 837 - 852 (2007/10/02)
Structure-activity relationships have been ascertained and chemical metodology developed for a series of antimalarial 3-chloroindoloquinoline-5-oxides.The basic side chain as well as the ring N-oxide are critical for antimalarial activity as is a bromine or chlorine in position 3.Substitution at positions 7,8,9,10 in not essential, although the most potent analog in our studies was the 8-nitro compound 4vv. indoloquinolines / antimalarial agents
Studies in Antifertility Agents: Part XXVII - Synthesis of 2-Acetyl-3-aryl-5-tosyl-7/8-H (or methoxy)-3,3a,4,5-tetrahydropyrazoloquinolines
Kelkar, Prabhakar M.,Sangwan, Naresh K.,Rastogi, Shri Nivas,Anand, Nitya
, p. 297 - 300 (2007/10/02)
N-Tosyl-2,3-dihydro-4-quinolones (12-14), prepared from aniline, m- and p-anisidines by reported procedures, on condensation with araldehydes in the presence of NaOMe give the corresponding 3-arylidene-4-quinolones (15-18).Refluxing of 15-18 with NH2-NH2*H2O in gl.AcOH affords the title compounds, 2-acetyl-3-aryl-5-tosyl-7/8-H (or methoxy)-3,3a,4,5-tetrahydropyrazoloquinolines (19-22).The stereochemistry of the title compounds based on the assignments of C3-H, C3a-H, C4-H2 protons has been studied by PMR decoupling experiments.In preliminary screening, compounds 19 and 22 have been found to prevent pregnancy at 20 mg/kg dose in female albino rats, but are ineffective at lower doses.None of the compounds tested shows any significant pharmacological activity.
