15818-13-0Relevant academic research and scientific papers
Electricity Driven 1,3-Oxohydroxylation of Donor-Acceptor Cyclopropanes: a Mild and Straightforward Access to β-Hydroxy Ketones
Banerjee, Prabal,Maajid Taily, Irshad,Saha, Debarshi
supporting information, p. 5053 - 5057 (2021/09/30)
An unprecedented external oxidant-free electrochemical protocol for 1, 3-oxohydroxylation of donor-acceptor cyclopropane is disclosed. The strategy encompasses the activation of the labile π-electron cloud of the aryl ring to cleave the strained Csp3?Csp3 bond of cyclopropane to afford the β-hydroxy ketones via insertion of molecular oxygen. More significantly, based on the detailed mechanistic investigations and cyclic voltammetry experiments, a plausible mechanism is proposed.
Preparation method of donepezil hydrochloride for treating Alzheimer's disease
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Paragraph 0036; 0037; 0043; 0049; 0055; 0057; 0059, (2017/10/05)
The invention discloses a preparation method of donepezil hydrochloride for treating the Alzheimer's disease. The preparation method comprises the following steps: (1) mixing 3,4-dimethoxy benzaldehyde with diethyl malonate, thus preparing a mixture M1 co
Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors
Lou, Jun,Yang, Xiaoyan,Rao, Zhigang,Qi, Wenwen,Li, Jinhui,Wang, Haiyu,Li, Yuxi,Li, Jinping,Wang, Zhiming,Hu, Xianming,Liu, Peng,Hong, Xuechuan
, p. 466 - 473 (2014/07/21)
A series of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives were prepared to evaluate their ability of inhibiting neuraminidase (NA) of influenza A virus. All the compounds were synthesized in good yields starting from aldehyde by using a suitable synthetic strategy, which showed moderate inhibitory activity against influenza A NA. Compound 6g exhibited the strongest inhibitory activity against influenza virus A NA (IC50 = 17.64 μM), which indicated pyrimidine ring could be used as a core structure to design novel influenza NA inhibitors.
Synthesis of novel 2, 5-dihydrofuran derivatives and evaluation of their anticancer activity
Zhang, Yikai,Zhong, Hanyu,Wang, Tiantian,Geng, Dongping,Zhang, Mingfeng,Li, Ke
scheme or table, p. 69 - 80 (2012/03/26)
According to metal-catalyzed [3 + 2] cycloaddition reaction, we synthesized a series of novel 2, 5-dihydrofuran derivatives and evaluated their in vitro anti-cancer activities via MTT method. The bioassay showed that the majority of the resultant compounds exerted anti-tumor effect against four human cancer cell lines to various extents, which supported the rationale of the design. Compounds 9e and 10g showed the highest activity with broad anti-cancer spectrum, which were good candidates for further evaluation.
Synthesis and anti-tumor activity of novel ethyl 3-aryl-4-oxo-3,3a,4,6- tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylates
Wang, Tiantian,Liu, Jia,Zhong, Hanyu,Chen, Huan,Lv, Zhiliang,Zhang, Yikai,Zhang, Mingfeng,Geng, Dongping,Niu, Chunjuan,Li, Yongmei,Li, Ke
scheme or table, p. 3381 - 3383 (2011/06/24)
A series of ethyl 3-aryl-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a- carboxylates were prepared through the metal-catalyzed domino reaction of alkylidene malonates and 1,4-butynediol under a one-pot reaction condition at room temperature. Their in vitro anti-proliferative activities were subsequently evaluated in A549, QGY and HeLa cells. The majority of the compounds showed potent anti-tumor activity against HeLa cells. In particular, compound 3l was the most potent compound with IC50 value of 5.4 μM. For the first time, the X-ray structure of the anti-tumor ethyl 3-aryl-4-oxo-3,3a,4,6- tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylates is determined.
5-PHENYL-3-PYRIDAZINONE DERIVATIVE
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Page/Page column 18, (2010/04/23)
To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases cau
5-phenyl-3-pyridazinone derivatives and drug composition containing the same
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, (2008/06/13)
A 5-phenyl-3-pyridazinone derivative having the formula (I) wherein R1represents an unsubstituted or substituted C1to C8alkyl group, C3to C7cycloalkyl group, or indanyl group; R2represents
A convenient synthesis of 3-arylbutanolides and 3-arylbutenolides
Gu, Jian-Xin,Holland, Herbert L.
, p. 3305 - 3315 (2007/10/03)
A series of 3-aryl-substituted butenolides and butanolides has been prepared in a common short synthetic sequence from the corresponding aryl aldehydes. The 3-arylbutanolides are prepared by cyclisation of 3-aryl-3- cyano-1-propanols, obtained by selectiv
Synthesis of 3-Aryl-1-tetralones
Selvaraj, S.,Rajendran, A. S.,Arumugam, N.
, p. 1047 - 1049 (2007/10/02)
A new method for the synthesis of 3-aryl-1-tetralones is presented.The tetralones synthesised have been characterised by elemental analysis and soectral data.
Reaction of Active Methylene Compounds with Veratraldehyde Schiff Bases and Antifungal Activity of Products
Manrao, M. R.,Kaur, Baljit,Sharma, R. C.,Kalsi, P. S.
, p. 1059 - 1060 (2007/10/02)
Michael reaction of veratraldehyde schiff bases with ethyl cyanoacetate, cyanoacetic acid, malonamide, acetylacetone, diethyl malonate, cyanoacetamide and malononitrile gives the addition elimination products, viz. ethyl 3,4-dimethoxybenzalcyanoacetate (2
