- Continuous flow photochemistry as an enabling synthetic technology: Synthesis of substituted-6(5: H)-phenanthridinones for use as poly(ADP-ribose) polymerase inhibitors
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Methods utilizing continuous flow photochemistry, an enabling synthetic technology, have been developed for the generation of phenanthridinones via an intramolecular photochemical cyclization of 2-chlorobenzamides for the purposes of generating poly(ADP-ribose) polymerase inhibitors. Herein we report 16 examples of a single-step flow photocyclization which produces substituted phenanthridinones in yields up to 99%, while a two-step method leads directly to phenanthridinones from 2-chlorobenzoyl chlorides and anilines via a novel continuous flow amidation/photocyclization protocol. Overall, the flow photocyclization reactions typically progress in good to excellent yields, and in a superior fashion to analogous batch methods, greatly enabling the drug discovery process.
- Fang,Tranmer
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supporting information
p. 720 - 724
(2016/05/19)
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- Copper catalysed C-N bond formation via a sequential acylation and deacylation process: A novel strategy for the synthesis of benzanilides
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An efficient and mild oxidative amidation of aldehydes by means of acetanilides as amine components has been developed for the first time using copper catalysis. The approach is versatile and proceeds through sequential acylation and deacylation steps to afford benzanilides.
- Kumar, Saurabh,Vanjari, Rajeshwer,Guntreddi, Tirumaleswararao,Singh, Krishna Nand
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p. 9920 - 9924
(2015/02/19)
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- Phosphine-free atmospheric carbonylation of aryl iodides with aniline derivatives in the presence of a reusable silica-supported palladium catalyst
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Various palladium catalysts were obtained by the immobilisation of palladium on silica, modified with imidazolium salts. The efficiency of the catalysts was greatly dependent on the choice of the anion of the imidazolium salt, the palladium precursor and on the conditions of heterogenisation. Palladium acetate immobilised on silica with grafted imidazolium chloride moieties was shown to be a selective and recyclable catalyst for atmospheric aminocarbonylation of aryl iodides with aromatic amines in DMF. It was proved that the greater loss of palladium in DMSO can be explained by the formation of soluble palladium complexes.
- Urbán, Béla,Papp, Máté,Srankó, Dávid,Skoda-F?ldes, Rita
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p. 150 - 157
(2015/02/19)
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- Highly efficient dehydrogenative cross-coupling of aldehydes with amines and alcohols
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A common protocol for the synthesis of amides, esters and α-ketoesters via cross dehydrogenative coupling of aldehydes and amines/alcohols has been developed. The method is applicable to a wide variety of alcohols and amines as well as aliphatic and aromatic aldehydes. Also, the use of acetaldehyde for acetylation and ethyl glyoxalate to access 2-oxo-amino esters is presented for the first time.
- Deshidi, Ramesh,Rizvi, Masood Ahmad,Shah, Bhahwal Ali
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p. 90521 - 90524
(2015/11/11)
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- Metal-free n -arylation of secondary amides at room temperature
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The arylation of secondary acyclic amides has been achieved with diaryliodonium salts under mild and metal-free conditions. The methodology has a wide scope, allows synthesis of tertiary amides with highly congested aryl moieties, and avoids the regioselectivity problems observed in reactions with (diacetoxyiodo)benzene.
- Tinnis, Fredrik,Stridfeldt, Elin,Lundberg, Helena,Adolfsson, Hans,Olofsson, Berit
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supporting information
p. 2688 - 2691
(2015/06/16)
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- Metal-free synthesis of amides by oxidative amidation of aldehydes with amines in PEG/oxidant system
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A simple, inexpensive, and efficient one-pot synthesis of amide derivatives were achieved in good to excellent yields via the directly oxidative amidation of aldehydes with amines under PEG/Oxidant system.
- Liang, Jun,Lv, Jing,Shang, Zhi-Cai
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supporting information; experimental part
p. 8532 - 8535
(2011/11/12)
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- SMALL MOLECULE MODIFIERS OF MICRORNA MIR-122
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MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new th
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Page/Page column 38; 40
(2011/08/08)
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- Small molecule modifiers of MicroRNA miR-122 function for the treatment of hepatitis C Virus infection and hepatocellular carcinoma
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MicroRNAs are a recently discovered new class of important endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation h
- Young, Douglas D.,Connelly, Colleen M.,Grohmann, Christoph,Deiters, Alexander
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supporting information; experimental part
p. 7976 - 7981
(2010/08/05)
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- Synthesis of amides through the Cannizzaro-type reaction catalyzed by lanthanide chlorides
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Amidation of aldehydes with lithium amides through the LnCl3-catalyzed Cannizzaro-type reactions afforded a variety of amides in high yields. The electronic and steric effects on the reaction were investigated. The features of the economical ca
- Zhang, Lijun,Su, Shunpeng,Wu, Hongping,Wang, Shaowu
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supporting information; experimental part
p. 10022 - 10024
(2010/02/27)
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- Synthesis of some aryl/heteroaryl tetrazole derivatives and their mass fragmentation study
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Synthesis of some aryl and heteroaryl tetrazole derivatives are described and their electron impact mass fragmentation pattern is discussed.
- Dutta, Babul C.,Borthakur, Susanta K.,Goswami, Birendra N.
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p. 565 - 568
(2007/10/03)
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- 1,3,4-Oxadiazolethiol as Acyl-transfer Reagent in Acylation of Amines: A One-pot Reaction
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Amines are acylated using 5-(2,4-dichlorophenyl)-1,3,4-oxadiazolethiol in the presence of diethyl chlorothiophosphate (DCTP) in good yield.
- Goswami,Borthakur,Ghosh
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p. 268 - 269
(2007/10/03)
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