- A highly diastereoselective oxa-Pictet-Spengler approach to (+)-astropaquinone B and (+)-astropaquinone C and the formation of astropaquinone B dimer
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A concise and highly diastereoselective synthesis of (+)-astropaquinone B and (+)-astropaquinone C is reported. The synthetic strategy is based on an efficient combination of Doetz benzannulation using a chiral alkyne to construct the naphthalene unit and
- Fernandes, Rodney A.,Mulay, Sandip V.
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- Practical and regioselective brominations of aromatic compounds using tetrabutylammonium peroxydisulfate
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Direct bromination of wide range of aromatic compounds substituted with electron donating groups such as methoxy, hydroxy, or amino groups have been achieved with high regioselectivity by the reaction with Br2 in the presence of tetrabutylammonium peroxydisulfate 1 under mild conditions in acetonitrile in excellent yields. The use of lithium bromide as a bromination reagent afforded high yields of monobromo compounds with complete regioselectivity under neutral and mild reaction conditions in acetonitrile.
- Park, Min Young,Yang, Seung Gak,Jadhav, Vidyadhar,Kim, Yong Hae
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- N-Bromosuccinimide as a Regioselective Nuclear Monobrominating Reagent for Phenols and Naphthols
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A wide range of substituted phenols and naphthols were regioselectively monobrominated with N-bromosuccinimide, at para position in acetonitrile and at ortho position in carbon disulfide, under mild conditions in good yields. Methylphenols afforded only nuclear bromination products.
- Carre?o, M. Carmen,García Ruano, José L.,Sanz, Gema,Toledo, Miguel A.,Urbano, Antonio
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- Practical and regioselective halogenations of aromatic compounds using tetrabutylammonium peroxydisulfate
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The halogenated aromatic compounds have been important intermediates for various synthetic methods. Electron-rich aromatic compounds were easily iodinated using tetrabutylammonium peroxydisulfate (1) and iodine in mild conditions with excellent yields. Bromination was achieved using 1 and bromine, and regioselective bromination of highly activated aromatic compounds was also achieved using 1 and lithium bromide in mild conditions with excellent yields. Copyright Taylor & Francis Inc.
- Min, Young Park,Seung, Gak Yang,Kim, Yong Hae
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- Copper(II) bromide: A simple and selective monobromination reagent for electron-rich aromatic compounds
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Copper(II) bromide was found to be a simple and efficient reagent for monobromination of electron-rich aromatic compounds at room temperature. The reaction proceeded smoothly with phenols, aryl alkyl ethers, and aromatic amines to afford the corresponding monobrominated product selectively in moderate to good yields. Copyright Taylor & Francis Group, LLC.
- Bhatt, Suchitra,Nayak, Sandip K.
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- Visible light-induced mono-bromination of arenes with BrCCl3
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A highly efficient and regioselective bromination of electron-rich arenes and heteroarenes using commercially available BrCCl3as a “Br” source has been developed. The reaction was performed in air under mild conditions with photocatalyst Ru(bpy)3Cl2·6H2O, avoiding the usage of strong acids and strong oxidants. Mono-brominated products were obtained with medium to excellent yields (up to 94%). This strategy has shown good compatibility and highpara-selectivity, which will facilitate the complicated synthesis.
- Fan, Jiali,Wei, Qiancheng,Zhu, Ershu,Gao, Jing,Cheng, Xiamin,Lu, Yongna,Loh, Teck-Peng
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supporting information
p. 5977 - 5980
(2021/06/18)
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- Synthesis method of 2-bromo-5-methoxyphenol
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The invention discloses a synthesis method of 2-bromo-5-methoxyphenol. According to the synthesis method, 3-methoxyphenol is taken as a raw material, firstly, the 3-methoxyphenol reacts with a protection reagent such as tert-butyldimethylsilyl chloride, a
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Paragraph 0096-0099
(2019/10/22)
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- Practical regioselective halogenation of vinylogous esters: Synthesis of differentiated mono-haloresorcinols and polyhalogenated resorcinols
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A practical and efficient method for the direct, regioselective conversion of vinylogous esters to haloresorcinols is reported. Control of the reaction conditions enables synthesis of either the 4- or 6-haloresorcinol isomers from a common precursor with excellent regiocontrol and high yield. The generality and functional group tolerance of this novel protocol is demonstrated. The utility of this methodology to access polyhaloresorcinols is also reported. These methods create useful functionalized building blocks for further synthetic applications.
- Chen, Xiaohong,Liu, Xiaoguang,Martinez, Jenny S.,Mohr, Justin T.
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p. 3653 - 3665
(2016/06/06)
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- Visible-light photoredox catalysis enabled bromination of phenols and alkenes
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A mild and efficient methodology for the bromination of phenols and alkenes has been developed utilizing visible light-induced photoredox catalysis. The bromine was generated in situ from the oxidation of Br- by Ru(bpy)33+, both of which resulted from the oxidative quenching process.
- Zhao, Yating,Li, Zhe,Yang, Chao,Lin, Run,Xia, Wujiong
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p. 622 - 627
(2014/04/17)
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- SUBSTITUTED PARA-BIPHENYLOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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The present invention relates to a series of substituted para-biphenyloxymethyl dihydro oxazolopyrimidinones of formula (I) as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of
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Page/Page column 82-83
(2011/04/19)
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- 5-MEMBERED HETEROARYL DERIVATIVES USED AS SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONISTS
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5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
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Page/Page column 36
(2011/01/12)
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- An enzymatically activated fluorescence probe for targeted tumor imaging
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β-Galactosidase is a widely used reporter enzyme, but although several substrates are available for in vitro detection, its application for in vivo optical imaging remains a challenge. To obtain a probe suitable for in vivo use, we modified our previously
- Kamiya, Mako,Kobayashi, Hisataka,Hama, Yukihiro,Koyama, Yoshinori,Bernardo, Marcelino,Nagano, Tetsuo,Choyke, Peter L.,Urano, Yasuteru
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p. 3918 - 3929
(2007/10/03)
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- Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists
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The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4′, R5, R5′, and R12 are as described in the specification.
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Page/Page column 19
(2010/11/08)
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- SEROTONERGIC BENZOFURANS
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The present invention provides serotonergic benzofurans of Formula (I): where A, R, R, R, R, and R are as described in the specification.
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Page/Page column 14
(2010/02/04)
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- ALKYLOXYAMINO SUBSTITUTED FLUORENONES AND THEIR USE AS PROTEIN KINASE C INHIBITORS
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The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).
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- 2-AMINO-6-(2-SUBSTITUTED-4-PHENOXY)-SUBSTITUTED-PYRIDINES
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This present invention relates to compounds of the formula wherein G, R1 and R2 are defined as in the specification, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.
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- Substrate regulation of product distribution in the reactions of aryl chromium carbene complexes with alkynes
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The reactions of arylcarbene complexes with alkynes were examined for six of the nine possible substitution patterns for mono- and dioxygenated aryl substituents of the carbene carbon. The product distributions were found to be highly dependent on a numbe
- Bos, Mary Ellen,Wulff, William D.,Miller, Ross A.,Chamberlin, Steven,Brandvold, Timothy A.
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p. 9293 - 9319
(2007/10/02)
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