- Copper-Catalyzed Enantioselective Hetero-Diels-Alder Reaction of Danishefsky's Diene with Glyoxals
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(Chemical Equation Presented) The highly enantioselective hetero-Diels-Alder reaction of Danishefsky's diene with glyoxals was developed by virtue of a readily accessible chiral copper catalyst. This efficient transformation provided a facile and scalable
- Li, Yanan,Hu, Yanbin,Zhang, Sheng,Sun, Jianan,Li, Lijun,Zha, Zhenggen,Wang, Zhiyong
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- Reactions of cyclohexyl isocyanide, dialkyl acetylenedicarboxylates and 1-aryl-2-ene-3-acetyl-1,4-diketones: One-pot synthesis of highly functionalized 5-cyclohexylimino-2,5-dihydrofurans
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Dihydrofurans are important intermediates in organic synthesis, and are also important starting materials used in syntheses of a number of natural products. A facile synthesis of highly functionalized 5- cyclohexylimino-2,5-dihydrofuran derivatives by the multi-component reaction of cyclohexyl isocyanide, dialkyl acetylenedicarboxylates and 1-aryl-2-ene-3-acetyl-1,4-diketones is described.
- Latifi, Mahsa,Talebdizaeh, Mahdiyeh,Anary-Abbasinejad, Mohammad
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- A 2 - cyano - 4 - chloro - 5 - (4 - methyl phenyl) imidazole synthesis method
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The invention relates to a synthetic method for 2-cyano-4-chloro-5-(4-methylphenyl)imidazole. The synthetic method comprises the following steps: (1) by taking p-methylacetophenone as a raw material, carrying out a halogenating reaction under a light condition to obtain a compound I; (2) dissolving the obtained compound I in a solvent, stirring the mixture to react at a certain temperature, and performing cooling and suction-filtering to obtain a compound II; (3) dissolving the obtained compound II in a solvent and carrying out a reaction with glyoxal and hydroxylamine sulphate at a certain temperature to obtain a compound III; and (4) dissolving the obtained compound III in a solvent, carrying out a reaction with sulfoxide chloride in an ice bath in a manner of raising the temperature to room temperature and keeping the temperature for the reaction, dropwise adding sulfur chloride, and after reaction, washing the product to obtain a compound IV which is 2-cyano-4-chloro-5-(4-methylphenyl)imidazole. The synthetic method is good in atom economy, simple and convenient in process operation and high in product yield and industrial application value.
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Paragraph 0035; 0040; 0045
(2017/11/01)
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- Metal free one-pot synthesis of α-ketoamides from terminal alkenes
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A practical approach towards the synthesis of α-ketoamides from readily available terminal alkenes (styrenes) has been developed. Use of inexpensive I2/2-iodoxybenzoic acid (IBX) in dimethyl sulphoxide (DMSO) as an oxidant under metal free one-pot conditions makes this methodology versatile.
- Dutta, Sayan,Kotha, Surya Srinivas,Sekar, Govindasamy
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p. 47265 - 47269
(2015/06/16)
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- PYRIDOPYRAZINES AS ANTICANCER AGENTS
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The present invention relates to pyridopyrazine derivatives and solvates, hydrates and pharmaceutically acceptable salts thereof, the use of them in the prevention and/or the treatment of cancer diseases, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the prevention and/or treatment of cancer diseases.˙
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Page/Page column 13
(2014/07/22)
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- Iodine-mediated oxidative annulation for one-pot synthesis of pyrazines and quinoxalines using a multipathway coupled domino strategy
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An efficient iodine-mediated oxidative annulation of aryl acetylenes-arylethenes-aromatic ketones with 1,2-diamines for the synthesis of pyrazines and regioselective synthesis of quinoxalines is presented. A multipathway coupled domino approach has been developed for the one-pot synthesis of 1,4-diazines with high functional group compatibility.
- Viswanadham, K. K. Durga Rao,Prathap Reddy, Muktapuram,Sathyanarayana, Pochampalli,Ravi, Owk,Kant, Ruchir,Bathula, Surendar Reddy
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supporting information
p. 13517 - 13520
(2015/01/09)
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- Design and synthesis of 2-acylbenzothiazoles via in situ cross-trapping strategy from benzothiazoles with aryl ketones
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An I2/KOH synergistically promoted direct ring-opening aroylation of benzothiazoles with aryl ketones has been discovered. Aryl ketones were seen to act as carbonyl sources to construct 2-acylbenzothiazoles. This reaction could provide an example for the convergent integration of self-labor domino sequences based on an in situ cross-trapping strategy.
- Gao, Qinghe,Wu, Xia,Jia, Fengcheng,Liu, Meicai,Zhu, Yanping,Cai, Qun,Wu, Anxin
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p. 2792 - 2797
(2013/04/24)
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- A multipathway coupled domino strategy: Metal-free oxidative cyclization for one-pot synthesis of 2-acylbenzothiazoles from multiform substrates
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A multipathway coupled domino strategy has been developed for the efficient synthesis of 2-acylbenzothiazoles from multiform substrates arylethenes, arylacetylenes, 2-hydroxy-aromatic ketones, and carbinols via four distinct pathways. Through a logical coupled oxidation/heterocyclization domino process, a variety of 2-acylbenzothiazoles were synthesized free of metal in one pot.
- Zhu, Yan-Ping,Jia, Feng-Cheng,Liu, Mei-Cai,Wu, An-Xin
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p. 4414 - 4417
(2012/10/29)
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- Synthesis of trisubstituted isoxazoles via in situ trapping strategy from α-nitro carbonyl compounds and methyl ketones or terminal aryl alkenes
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A highly efficient domino method for the synthesis of trisubstituted isoxazoles has been established from α-nitro carbonyl compounds and methyl ketones or terminal aryl alkenes. Simple and readily available starting materials, mild reaction conditions and very simple operation are significant advantages of the reaction.
- Yang, Yan,Gao, Meng,Deng, Cong,Zhang, Dong-Xue,Wu, Liu-Ming,Shu, Wen-Ming,Wu, An-Xin
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supporting information; experimental part
p. 6257 - 6262
(2012/08/28)
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- Selective oxidation of benzylic or allylic hydroxyl group of sec-1,2-diols
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A mild and efficient method to selectively oxidize chiral sec-1,2-diols has been developed, which demonstrates that 2,3-dichloro-5,6-dicyano-1,4- benzoquinone (DDQ) can selectively oxidize benzylic or allylic hydroxyl group of sec-1,2-diols under ultrasound wave promotion. The configuration of the adjacent chiral center is retained.
- Peng, Kun,Chen, Fuxin,She, Xuegong,Yang, Chunhui,Cui, Yuxin,Pan, Xinfu
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p. 1217 - 1220
(2007/10/03)
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- Inhibitors of anthrax lethal factor activity
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Methods and compositions that act as specific inhibitors of ALF activity for the prophylaxis and treatment of anthrax infections.
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- A New Synthetic Route to Aromatic Gyloxals
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Dichloroacylation of toluene, o- and m- xylenes, chloro- and bromo-benzenes and m-chlorotoluene under Friedel-Crafts conditions leads to the corresponding chloroketones (Ia-f) which on controlled hydrolysis afford the glyoxals (IIa-f) respectively.
- Mahato, S. B.,Podder, G.,Maitra, S. K.
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- THE PREPARATION OF ARYLGLYOXALS AND HETEROAROMATIC ALDEHYDES USING PYRIDONA
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Aodium 1-oxido-4,6-diphenyl-2-pyridone reacts with phenacyl halides to give arylglyoxals and with N-heteroarylmethylpyridinium cations to give heteroaromatic aldehydes and ketones.
- Katritzky, A. R.,Chapman, A. V.,Dowlatshahi, H. M.
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p. 315 - 320
(2007/10/02)
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