4837-90-5Relevant articles and documents
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs
Lebar, Matthew D.,Hahn, Kristopher N.,Mutka, Tina,Maignan, Patrick,McClintock, James B.,Amsler, Charles D.,Van Olphen, Alberto,Kyle, Dennis E.,Baker, Bill J.
, p. 5756 - 5762 (2011)
The marine invertebrate-derived meridianin A, the originally proposed structure for psammopemmin A, and several related 3-pyrimidylindole analogs were synthesized and subsequently investigated for central nervous system, antimalarial, and cytotoxic activity. A Suzuki coupling of an indoleborate ester to the pyrimidine electrophile was utilized to form the natural product and derivatives thereof. The 3-pyrimidineindoles were found to prevent radioligand binding to several CNS receptors and transporters, most notably, serotonin receptors (i for 5HT2B). Two compounds also inhibited the human malaria parasite Plasmodium falciparum (IC50 50 = 15 μM).
Potassium tert-Butoxide-Promoted Acceptorless Dehydrogenation of N-Heterocycles
Liu, Tingting,Wu, Kaikai,Wang, Liandi,Yu, Zhengkun
supporting information, p. 3958 - 3964 (2019/08/01)
Potassium tert-butoxide-promoted acceptorless dehydrogenation of N-heterocycles was efficiently realized for the generation of N-heteroarenes and hydrogen gas under transition-metal-free conditions. In the presence of KOtBu base, a variety of six- and five-membered N-heterocyclic compounds efficiently underwent acceptorless dehydrogenation to afford the corresponding N-heteroarenes and H2 gas in o-xylene at 140 °C. The present protocol provides a convenient route to aromatic nitrogen-containing compounds and H2 gas. (Figure presented.).
Preparation method of 4-hydroxyindole
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Paragraph 0018-0020; 0025-0027; 0032-0034; 0039-0048, (2018/05/16)
The invention discloses a preparation method of 4-hydroxyindole, comprising the steps of (1) dissolving 3-methoxyphenylhydrazine hydrochloride in DMF (dimethylformamide), adding concentrated sulfuricacid and a catalyst, mixing well, adding acetaldehyde, allowing reflux reaction at controlled temperature of 60-80 DEG C for 90-120 min, filtering after reaction is over to obtain 4-methoxyindole; (2)dissolving 4-methoxyindole in dichloromethane, adding the obtained solution in a reactor, introducing nitrogen, controlling the temperature to 50-70 DEG C, and introducing HBr into the solution, allowing reflux reaction for 45-90 min, lowering the temperature to room temperature, performing reduced pressure removal of a solvent, and recrystallizing to obtain 4-hydroxyindole. The preparation method according to the application is simple to perform and has mild conditions and few byproducts, the product is high in purity, and the yield of the product is high.