15982-61-3Relevant academic research and scientific papers
Design and synthesis of novel triazole linked pyrrole derivatives as potent Mycobacterium tuberculosis inhibitors
Devi, M. Lakshmi,Reddy, P. Lakshmi,Yogeeswari,Sriram,Reddy, T. Veera,Reddy, B. V. Subba,Narender
, p. 2985 - 2999 (2017)
This research is focused on the rational approach to design and synthesis of a novel series of triazole linked pyrrole derivatives through a sequential Paal–Knorr reaction and Click chemistry. These new molecules were screened against Mycobacterium tuberculosis H37Rv and found to display promising anti-mycobacterial activity. Among various compounds, 7g and 7l were identified as leads with minimum inhibitory concentration value 0.78 (μg/mL), which are more effective than standard drugs such as pyrazinamide, ethambutol, and ciprofloxacin and less active than isoniazid and rifampicin. These molecules (minimum inhibitory concentration values 12.5 μg/mL) were also screened against HEK-293T cancer cell lines. Most of these molecules are less toxic but possess higher selectivity index, which indicates the suitability of these compounds for further evaluation.
Visible-Light-Promoted Photocatalyst-Free Hydroacylation and Diacylation of Alkenes Tuned by NiCl2·DME
Zhao, Xinxin,Li, Bing,Xia, Wujiong
, p. 1056 - 1061 (2020/02/15)
Herein, we describe a visible light-promoted hydroacylation strategy that facilitates the preparation of ketones from alkenes and 4-acyl-1,4-dihydropyridines via an acyl radical addition and hydrogen atom transfer pathway under photocatalyst-free conditions. The efficiency was highlighted by wide substrate scope, good to high yields, successful scale-up experiments, and expedient preparation of highly functionalized ketone derivatives. In addition, this protocol allows for the synthesis of 1,4-dicarbonyl compounds through alkene diacylation in the presence of NiCl2·DME.
Samarium-promoted michael addition between aroyl chlorides and chalcones
Liu, Yongjun,Li, Yuanying,Qi, Yan,Wan, Jun
experimental part, p. 4188 - 4192 (2011/02/25)
A novel Michael addition type reaction between aroyl chlorides and chalcones was realized in the presence of samarium metal when N,N-dimethylformamide was used as a solvent. A variety of 1,4-diketones were thereby synthesized in moderate to good yields. T
Photoaccelerated reductive coupling of acid chlorides with conjugate dienes and styrenes by use of neodymium metal in N,N-dimethylacetamide
Li, Zhi-Fang,Tomisaka, Yuri,Nomoto, Akihiro,Zhang, Yongmin,Ogawa, Akiya
body text, p. 16 - 17 (2009/12/02)
Upon photoirradiation, neodymium metal powder in N,N-dimethylacetamide (DMAC) exhibits excellent reducing ability for the reductive coupling of benzoyl chlorides with conjugate dienes and styrenes. Copyright
A new method for the synthesis of acyltitanium complexes and their application to copper-mediated acylmetallation of carbon-carbon multiple bonds in aqueous media
Han, Zhenfu,Fujioka, Takuma,Usugi, Shin-Ichi,Yorimitsu, Hideki,Shinokubo, Hiroshi,Oshima, Koichiro
, p. 1622 - 1623 (2007/10/03)
Treatment of α,β-unsaturated carbonyl compounds or methyl propargyl ether with acylchlorobis(cyclopentadienyl)titanium in the presence of Methylamine and a copper salt in aqueous THF resulted in acylation of the carbon-carbon multiple bond, yielding the c
Formation of 1,4-diketones via bis-acylation of the conjugated carbon-carbon double bonds in acrylates, acrylamides, methyl vinyl ketone and styrenes with aroyl chlorides promoted by samarium metal in DMF
Liu, Yongjun,Zhang, Yongmin
, p. 8429 - 8437 (2007/10/03)
Promoted by samarium in DMF, aroyl chlorides react readily with conjugated carbon-carbon double bonds in acrylates, acrylamides, methyl vinyl ketone and styrenes in a bis-acylation manner. These reactions proceed smoothly under mild conditions without the need of pretreating or activating the metallic samarium, affording the corresponding 1,4-diketones in good to excellent yields.
Reactions of 2-(Dialkylamino)arylacetonitriles with Acetylenes Under Basic Conditions. A Simple Synthesis of Substituted Mono and Diketones
Zdrojewski, T.,Jonczyk, A.
, p. 224 - 233 (2007/10/02)
2-(Dialkylamino)arylacetonitriles 1 react with acetylenes 2a,b in dimethyl sulfoxide, powdered sodium hydroxide and triethylbenzylammonium chloride as a catalyst to give 3 and/or 4.The latter are formed via addition of anion 8 to immonium salt 9.The type of product formed depends on the basicity of amino moiety in 3.Furthermore, compound 1 adds to C-1 of acetylene 2c affording the vinyl derivatives 15.The products 3,4,11 and 15 are hydrolyzed to give ketones 5-7,12 and 16, respectively.
Enone Synthesis via Palladium Catalyzed Reductive Carbonylation of Terminal Acetylenes
Tamaru, Yoshinao,Ochiai, Hirofumi,Yoshida, Zen-ichi
, p. 3861 - 3864 (2007/10/02)
Aryl vinyl ketones are prepared by the reaction of aryl iodides and terminal acetylenes in the presence of a catalytic amount of PdCl2(PPh3)2, Cp2TiCl2 and a stoichiometric amount of Zn-Cu under an atmospheric pressure of carbon monoxide.
