96013-75-1Relevant academic research and scientific papers
Synthesis of New Tyrosol-Based Phosphodiester Derivatives: Effect on Amyloid β Aggregation and Metal Chelation Ability
Romanucci, Valeria,Giordano, Maddalena,De Tommaso, Gaetano,Iuliano, Mauro,Bernini, Roberta,Clemente, Mariangela,Garcia-Vi?uales, Sara,Milardi, Danilo,Zarrelli, Armando,Di Fabio, Giovanni
, p. 1172 - 1183 (2021/02/01)
Alzheimer's disease (AD) is a multifactorial pathology that requires multifaceted agents able to address its peculiar nature. Increasing evidence has shown that aggregation of amyloid β (Aβ) and oxidative stress are strictly interconnected, and their modu
Pyrazine compounds with multiple effects and preparation method thereof
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Paragraph 0056-0057; 0060-0061, (2020/11/01)
The invention relates to pyrazine compounds, stereoisomers, tautomers and pharmaceutically acceptable salts of the pyrazine compounds. The pyrazine compounds can be used for treating Alzheimer's disease, Parkinson's disease, Huntington's disease, frontal temporal dementia (FTD), vascular dementia, HIV-related dementia, multiple sclerosis, progressive spinal cord lateral sclerosis, Friedel-Crafts ataxia, neuropathic pain or glaucoma and other neurodegenerative diseases, diabetes mellitus and related diabetic complications, inflammation, oxidative damage and mitochondria-related diseases.
Pyrazine compound and preparation method thereof
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Paragraph 0060; 0063-0064, (2020/11/09)
The invention relates to a pyrazine compound, a stereoisomer, a tautomer and a pharmaceutically acceptable salt thereof, wherein the pyrazine compound, the stereoisomer, the tautomer and the pharmaceutically acceptable salt thereof can treat Alzheimer's disease, Parkinson's disease, Huntington's disease, frontal temporal dementia (FTD), vascular dementia, HIV-related dementia, multiple sclerosis,progressive spinal cord lateral sclerosis, Friedel-Crafts ataxia, neuropathic pain or glaucoma and other neurodegenerative diseases, diabetes mellitus and related diabetic complications, inflammations, oxidative damage and mitochondria-related diseases.
Application of pyrazine compound in preparation of drugs
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Paragraph 0063; 0066-0067, (2020/10/30)
The invention relates to an application of a pyrazine compound in preparation of drugs. The drugs can be used for treating neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, frontotemporal dementia (FTD), vascular dementia, HIV-related dementia, multiple sclerosis, progressive lateral sclerosis, Friedreich's ataxia, neuropathic pain or glaucoma, inflammation, oxidative damage, and mitochondrial-related diseases.
Deoxyfluorination with CuF2: Enabled by Using a Lewis Base Activating Group
Bode, Bela E.,Chabbra, Sonia,Champion, Sue,Dawson, Daniel M.,Sood, D. Eilidh,Sutherland, Andrew,Watson, Allan J. B.
supporting information, p. 8460 - 8463 (2020/04/10)
Deoxyfluorination is a primary method for the formation of C?F bonds. Bespoke reagents are commonly used because of issues associated with the low reactivity of metal fluorides. Reported here is the development of a simple strategy for deoxyfluorination, using first-row transition-metal fluorides, and it overcomes these limitations. Using CuF2 as an exemplar, activation of an O-alkylisourea adduct, formed in situ, allows effective nucleophilic fluoride transfer to a range of primary and secondary alcohols. Spectroscopic investigations have been used to probe the origin of the enhanced reactivity of CuF2. The utility of the process in enabling 18F-radiolabeling is also presented.
A deprotection procedure using SO3H silica gel to remove non-silyl protecting groups
Karaki, Fumika,Kuwada, Miki,Tajiri, Saki,Kanda, Misaki,Yanai, Mari,Kamimura, Mitsuhiro,Itoh, Kennosuke,Fujii, Hideaki
supporting information, p. 212 - 220 (2019/05/06)
Protecting groups are indispensable in organic synthesis and there is a great need for a variety of deprotection methods. Here, we investigated the scope of the application of a deprotection procedure using SO3H silica gel, which we have previously reported as a desilylation procedure. Under these conditions, -OMOM, -OSEM, -OTHP, and -OAc groups and dimethyl acetal were cleaved. Pivaloyloxy, benzyloxy and methoxy carbonyl groups remained intact and selective deprotection of TBS groups in the presence of other protecting groups was accomplished. We succeeded in cleaving an acetyl group on a secondary alcohol in a highly polar nortropine derivative. Our findings here provide another deprotection option and would be helpful in the synthesis of multifunctional compounds.
Tandem Oxidative Dearomatizing Spirocyclizations of Propargyl Guanidines and Ureas
Singh, Ravi P.,Das, Jayanta,Yousufuddin, Muhammed,Gout, Delphine,Lovely, Carl J.
, p. 4110 - 4113 (2017/08/15)
Treatment of propargyl ureas or guanidines with iodosobenzene diacetate results in an oxidative tandem amination/etherification dearomatizing spirocyclization. This transformation leads directly to the complete framework of the Leucetta alkaloids, spiroca
Synthesis and biological evaluation of analogs of AAL(S) for use as ceramide synthase 1 inhibitors
Toop, Hamish D.,Don, Anthony S.,Morris, Jonathan C.
, p. 11593 - 11596 (2015/12/08)
A convergent synthesis to access hydrophobic tail analogs and head group modifications of AAL(S) is described. The analogs synthesised were evaluated for their ability to inhibit ceramide synthase 1 and for their cytotoxicity in K562 cells. Our results ha
Stereoselective synthesis of bioactive natural spiroacetals aculeatins A and B
Das, Biswanath,Krishnaiah, Martha,Sudhakar, Chithaluri
scheme or table, p. 2303 - 2305 (2010/07/04)
The stereoselective synthesis of two naturally occurring bioactive spiroacetals, aculeatins A and B has been accomplished using 1-tetradecanal as the starting material. The sequence introduces diastereoselective iodine-induced electrophilic cyclization an
A novel, chemoselective and efficient microwave-assisted deprotection of silyl ethers with Selectfluor
Shah, Syed Tasadaque A.,Singh, Surendra,Guiry, Patrick J.
experimental part, p. 2179 - 2182 (2009/07/01)
A novel microwave-assisted, chemoselective and efficient method for the cleavage of silyl ethers (aliphatic and aromatic) catalyzed by Selectfluor is reported. A wide range of TBS-, TIPS-, and TBDPS-protected alkyl silyl ethers can be chemoselectively cleaved in high yield in the presence of aryl silyl ethers. The chemoselective deprotection of phenolic TBS ethers, and not the TIPS- or TBDPS-protected phenolic ethers, and the deprotection of silyl esters were also achieved under these reaction conditions. In addition, the transetherification and etherification of benzylic hydroxy groups in alcoholic solvents is observed.
