- PIFA-Mediated Cross-Dehydrogenative Coupling of N-Heteroarenes with Cyclic Ethers: Ethanol as an Efficient Promoter
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Ethanol is typically used in organic synthesis as an environmentally benign solvent. Herein, we report a mild and efficient cross-dehydrogenative coupling (CDC) reaction of N-heteroarenes with cyclic ethers by uncovering the new reactivity of ethanol as an efficient promoter in PIFA-mediated radical process. The reaction proceeds smoothly under the irradiation of visible light and features excellent functional group compatibility, which allows the expedite synthesis of a variety of medicinally valuable Cα-heteroarylated cyclic ethers in moderate to high yields.
- Li, Xiang,Liu, Chaoyang,Guo, Shixun,Wang, Wei,Zhang, Yongqiang
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- Carbon nitride as a heterogeneous visible-light photocatalyst for the Minisci reaction and coupling to H2 production
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Cyanamide functionalised carbon nitride powder is reported as a photocatalyst for direct Minisci-type coupling of heteroarenes with ethers, alcohols, and amides using atmospheric oxygen as the oxidant at room temperature. This mild protocol displays broad substrate scope, good functional group tolerance and the catalyst can be easily isolated and reused for several cycles. It thereby addresses the two major limitations of previously reported photoredox-mediated Minisci reactions: (i) use of expensive and potentially harmful non-recyclable photocatalysts, and (ii) requirement of a stoichiometric amount of strong chemical oxidant. Finally, using platinum as a co-catalyst with the carbon nitride allows this light-mediated reaction to generate two value-added products under an anaerobic atmosphere-functionalised heteroarenes and H2 fuel.
- Vijeta, Arjun,Reisner, Erwin
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- INHIBITORS OF MLH1 AND/OR PMS2 FOR CANCER TREATMENT
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The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R1, R2, R3, R4, R6
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Paragraph 00513-00514
(2021/12/28)
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- Heteroarylation of Ethers, Amides, and Alcohols with Light and O2
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An efficient protocol for the Cα-H heteroarylation of ethers, amides, and alcohols using air and light under mild conditions is described. The reaction is applicable to a wide spectrum of functional groups. The generation of C-radicals via photoinduced aerobic oxidation of ethers, amides, and alcohols is the key feature of the process. Control experiments suggest a radical pathway for the reaction.
- Bhakat, Manotosh,Biswas, Promita,Dey, Jayanta,Guin, Joyram
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supporting information
p. 6886 - 6890
(2021/09/14)
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- ADENOSINE RECEPTOR BINDING COMPOUNDS
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The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
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Paragraph 00660-00661
(2020/02/06)
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- BIS1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES AND THEIR USES AS PHARMACEUTICALS
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Use of Bis 1,2,3,4-tetrahydroisoquinoline derivatives represented by formula (I) as SK channel blockers and for the preparation of a medicament useful for the treatment of disorders of the central nervous system.
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Page/Page column 7
(2009/04/24)
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- Samarium-promoted coupling of pyridine-based heteroaryl analogues of benzylic acetates with carbonyl compounds
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(Chemical Equation Presented) 2-Substituted pyridine, quinoline, isoquinoline, bipyridine, and 1,10-phenanthroline analogues of benzylic acetates undergo Sml2-promoted coupling with aldehydes and ketones to afford (2-hydroxyalkyl)heteroaromatics.
- Weitgenant, Jeremy A.,Mortison, Jonathan D.,Helquist, Paul
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p. 3609 - 3612
(2007/10/03)
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- A new, convenient, highly selective free-radical hydroxymethylation of heteroaromatic bases by persulfate oxidation of ethylene glycol and glycerol, catalysed by AgNO3
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A new, convenient and selective source of hydroxymethyl ( .CH2OH) radical has been developed by persulfate oxidation of ethylene glycol with AgNO3 catalysis. The .CH 2OH radical is selectively trapped
- Minisci, Francesco,Porta, Ombretta,Recupero, Francesco,Punta, Carlo,Gambarotti, Cristian,Pruna, Barbara,Pierini, Monica,Fontana, Francesca
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p. 874 - 876
(2007/10/03)
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- ELECTROCHEMICAL REDUCTION OF PRISTINAMYCIN IA AND RELATED STREPTOGRAMINS IN AQUEOUS ACIDIC MEDIUM
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The electrochemical reduction of the picolinoyl residue of pristinamycinIA and related streptogramins was performed at a mercury cathode, in aqueous medium.The presence of a peptidic lactone residue at the amide nitrogen atom markedly modified the expected cathodic behaviour of pyridyl carboxamides: in particular, we observed the reduction of the pyridyl ring into tetrahydropyridine derivatives.Thanks to a series of model heterocyclic carboxamides, increasing steric hindrance at the amide nitrogen position was shown to lead to enhanced reduction of the heterocyclic ring.
- Largeron, M.,Vuilhorgne, M.,Potier, I. Le,Auzeil, N.,Bacque, E.,and al.
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p. 6307 - 6332
(2007/10/02)
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- COMPOUNDS WITH BRIDGEHEAD NITROGEN PART 74. NMR SPECTRA AND STEREOCHEMISTRY OF 1,3,10,10a-TETRAHYDRO-5H-OXAZOLOISOQUINOLINE AND 1,5,6,10b-TETRAHYDRO-3H-OXAZOLOISOQUINOLINE
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Whereas 1,3,10,10a-tetrahydro-5H-oxazoloisoquinoline adopts an equilibrium in CDCl3 solution at 295 K in which the trans-fused conformation predominates, 1,5,6,10b-tetrahydro-3H-oxazoloisoquinoline adopts the O-inside cis-fused conformation.This difference in conformational preference has been explained partly in terms of ring-fusion strain.
- Crabb, Trevor A.,Patel, Asmita V.
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p. 431 - 440
(2007/10/02)
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- Triazolopyridines. Part 5. The Reactions of 1,2,3-Triazoloisoquinoline: A New Route to 1,3-Disubstituted Isoquinolines
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Substitution of 1,2,3-triazoloisoquinoline by electrophiles occurs at position 1, lithiation at position 5.The lithio derivative (8) reacts with electrophiles to give 5-substituted derivatives (9)-(13).Hydrolytic ring opening of compound (4) and of compound (9) occurs with loss of nitrogen, thus providing a synthesis of 1,3-disubstituted isoquinolines.The conversion of a 3,4-disubstituted triazoloquinoline into a 2,3-disubstituted derivative of quinoline is described.A direct synthesis of N,N-dialkylquinolyl- (21) and N,N-dialkylisoquinolyl-acetamides (24) and (25) and the conversion of compound (21) into N,N-diethyltriazoloquinoline-4-carboxamide (3) has been achieved.
- Abarca, Belen,Bellesteros, Rafael,Gomez-Aldaravi, Estrella,Jones, Gurnos
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p. 1897 - 1902
(2007/10/02)
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- PHARMACOLOGICALLY ACTIVE TRIAZINONES
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The compounds are substituted 1,2,4-triazin-5-ones which are histamine H 2-antagonists. Two specific compounds of the present invention are 3-2-(5-methyl-4-imidazolylmethylthio)ethylamino!-6-(3-methoxybenzyl)-1,2, 4-tr iazin-5-one and 3-2-(5-methyl-4-imidazolylmethylthio)ethylamino!-6-(3-pyridylmethyl)-1,2,4-tr iazin-5-one.
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