110912-15-7Relevant articles and documents
Efficient synthesis of some new antiproliferative N-fused indoles and isoquinolines via 1,3-dipolar cycloaddition reaction in an ionic liquid
Sutariya, Tushar R.,Labana, Balvantsingh M.,Parmar, Narsidas J.,Kant, Rajni,Gupta, Vivek K.,Plata, Gabriela B.,Padrón, José M.
, p. 2657 - 2668 (2015)
Syntheses of some new pyrrolo-fused pyrrolo[1,2-a] indole derivatives have been achieved by combining N-allyl-indole-2-carbaldehyde with a variety of N-alkyl-glycine esters as well as tetrahydroisoquinolines in an ionic liquid, triethylammonium acetate (TEAA), a recyclable reaction medium, via intramolecular [3+2] cycloaddition reaction. This new method is highly efficient, and the ionic liquid employed is recyclable. The stereochemistry of all the compounds was confirmed by 2D NMR NOESY and in some cases single crystal X-ray diffraction data. The in vitro screening of all new candidates against various bacterial strains and representative human solid tumor cell lines, A549 (lung), HeLa (cervix), SW1573 (lung), T-47D (breast) and WiDr (colon), revealed that many of them have good antibacterial, antifungal and antitubercular and antiproliferative activities.
Synthesis of some heterocyclic compounds derived from indole as antimicrobial agents
Sayed, Mostafa,Kamal El-Dean, Adel M.,Ahmed, Mostafa,Hassanien, Reda
, p. 413 - 421 (2018)
Recently, indoles are considered interesting heterocyclic compounds due to their wide range of biological activities such as antimicrobial activity. Herein, some new indole derivatives containing heterocyclic moieties were synthesized using 3-chloro-1H-Indole-2-carbaldehyde (1) as a starting material, then allowed to react with compounds containing active methylene under Knoevenagel condensation and afforded the corresponding compounds (2, 3, 9). Also, the compound (1) when allowed to react with hydrazine derivatives gave the corresponding thiosemiccarbazone, semicarbazone, and hydrazone derivatives (4, 5, 6). Reaction of thiosemicarbazone derivatives with α-halognated carbonyl compounds gave the thiazolyl indole derivatives (10, 12a–b). Cyclic chalcones (11a–c) were obtained when compound (10) reacted with different aromatic aldehydes. The structures of all new synthesized compounds were confirmed on the basis of spectral analysis, IR, 1H NMR, 13C NMR, and MS spectroscopy. All synthesized compounds were evaluated for their antimicrobial activity. Compounds (2, 5, 7, 8, 11a, 12a) showed high antibacterial activity and compounds (3, 6, 9, 10, 11a, 12a) showed high antifungal activity.
Efficient preparation method of 3-substitued-benzo five-membered heterocycle-2-carbonyl compound
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Paragraph 0059-0061, (2017/08/30)
The invention discloses an efficient compounding method of a 3-substitued-benzo five-membered heterocycle-2-carbonyl compound. According to the method, a 3-substitued-benzo five-membered heterocycle-2-alcohol compound is subjected to a halogenated oxidation reaction by a halogenating reagent to generate the corresponding 3-substitued-benzo five-membered heterocycle-2-carbonyl compound. The efficient compounding method has the advantages that raw materials are easy to get, reaction conditions are mild, and reaction selectively and yield are high.