2677-05-6Relevant academic research and scientific papers
Fluorine-substituted bimolecular carbazole derivative as well as preparation method and application thereof
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Paragraph 0059-0069, (2020/07/08)
The invention discloses a fluorine-substituted bimolecular carbazole derivative represented by a formula (I) or pharmaceutically acceptable salt thereof. R1, R2, R3, R4 and R5 are defined in the specification. The fluorine-substituted bimolecular carbazole derivative or the pharmaceutically acceptable salt thereof provided by the invention can be used for preparing a DNA methyltransferase inhibitor or a histone demethylase inhibitor, and in-vitro cancer cell anti-proliferation tests prove that the fluorine-substituted bimolecular carbazole derivative has anti-proliferation activity on cancer cells.
Fluorine-substituted monocarbazole derivative as well as preparation method and application thereof (by machine translation)
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Paragraph 0087-0093, (2020/06/20)
The invention belongs to the field of pharmaceutical chemistry, and relates to a fluorine-substituted monocarbazole derivative which is one or more of compounds represented by formula (I) and formula (II) or a pharmaceutically acceptable soluble salt formed by a compound represented by formula (II). The fluorine-substituted monocarbazole derivatives obtained in the application can be used for preparing DNA methyltransferase inhibitors or histone demethylase inhibitors. The fluorine-substituted monocarbazole derivative has an inhibitory effect on the proliferation of cancer cells and can be used for preparing medicaments for treating and/or preventing cancer. An in-vitro cancer cell proliferation inhibition test shows that the fluorine-substituted monocarbazole compound obtained by the invention shows anti-proliferation activity against human lung cancer cells (A549), human colon cancer cells (HCTCTCT116), human gastric cancer cells (MNK NK NK-45), human liver cancer cells (HepepepG2), RPMI PMI PMI PMI PMI PMI and Karpppp289. (by machine translation)
N-heterocyclic carbene-Pd(II)-2-methyl-4,5-dihydrooxazole complex-catalyzed highly chemoselective mono-amination of dichlorobenzenes
He, Qian-Wei,Lu, Jian-Mei,Shao, Li-Xiong,Sun, Kai-Xin,Zhou, Jin-Hui
, (2020/01/22)
The palladium-catalyzed chemoselective mono-amination of dichlorobenzenes was reported in this paper. Under the suitable conditions, all reactions involving the three isomers of dichlorobenzenes with various secondary and primary amines in the presence of
Palladium C-N bond formation catalysed by air-stable robust polydentate ferrocenylphosphines: A comparative study for the efficient and selective coupling of aniline derivatives to dichloroarene
Platon, Melanie,Roger, Julien,Royer, Sylviane,Hierso, Jean-Cyrille
, p. 2072 - 2080 (2014/06/24)
The arylation of aniline derivatives with dichloroarenes under a low palladium content (below the currently used 5 to 10 mol%) was studied using nine different ferrocenylphosphine ligands, including the easily accessible 1,1′-bis(diphenylphosphino)ferrocene, DPPF. The electron-enriched air-stable tridentate ferrocenylpolyphosphine 1,2-bis(diphenylphosphino)- 1′-(diisopropylphosphino)-4-tert-butylferrocene, L5, employed in 2 mol% in combination with 1 mol% [PdCl(η3-C3H 5)]2 allows an efficient and selective coupling, while such demanding substrates currently induce chloroarene homocoupling and/or dehalogenation processes. The scope and limitation of the optimized system are explored, with a focus on electron-poor fluoroanilines (deactivated nucleophiles) and electron-rich methylated and methoxylated dichlorobenzenes (deactivated electrophiles). The Royal Society of Chemistry 2014.
Photoinduced cleavage of N-N bonds of aromatic hydrazines and hydrazides by visible light
Zhu, Mingzhao,Zheng, Nan
, p. 2223 - 2236 (2011/09/15)
A photocatalytic system involving [Ru(bpyrz)(PFH, visible light, and air has been developed for cleavage of the N-N bonds of hydrazines and hydrazides. This catalytic system is generally effective for N,N-disubstituted hydrazine and hydrazide derivatives, including arylhydrazides, N-alkyl-N-arylhydrazines, and N,N-diarylhydrazines. The utility of this cleavage reaction has been demonstrated by synthesizing a variety of secondary aromatic amines. Georg Thieme Verlag Stuttgart ? New York.
Intramolecular direct arylation in the synthesis of fluorinated carbazoles
Bedford, Robin B.,Betham, Michael,Charmant, Jonathan P.H.,Weeks, Amanda L.
, p. 6038 - 6050 (2008/12/20)
The amination of 2-chloroanilines with aryl bromides and subsequent intramolecular direct arylation can be exploited in the synthesis of a range of fluorinated carbazoles, where the fluorine substituent can be introduced via the aniline, the aryl bromide or both substrates. Depending on substitution patterns, the two steps can either be performed in tandem in one-pot under microwave heating conditions or else require a two pot approach.
