13303-10-1Relevant academic research and scientific papers
Synthesis method of N-BOC-ethylenediamine
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Paragraph 0025-0026, (2021/06/22)
The invention provides a synthesis method of N-BOC-ethylenediamine. The synthesis method of the N-BOC-ethylenediamine is characterized in that ethylenediamine and tert-butyl (p-nitrophenyl) carbonate (namely a self-made compound A) are subjected to a reac
MgBr 2 · OEt 2: A Lewis Acid Catalyst for the O - And N -Boc Protection of Phenols and Amines
Schechter, Aaron,Goldrich, David,Chapman, Jessica R.,Uberheide, Beatrix M.,Lim, Daniel
supporting information, p. 653 - 660 (2015/10/29)
MgBr2 · OEt2 efficiently catalyzes the O- and N-tert-butoxycarbonylation of functionalized phenols and amines. The presented procedure is operationally simple and done under solvent-free conditions. GRAPHICAL ABSTRACT.
Development of potent and selective tissue transglutaminase inhibitors: Their effect on TG2 function and application in pathological conditions
Badarau, Eduard,Wang, Zhuo,Rathbone, Dan L.,Costanzi, Andrea,Thibault, Thomas,Murdoch, Colin E.,El Alaoui, Said,Bartkeviciute, Milda,Griffin, Martin
, p. 1347 - 1361 (2015/12/26)
Potent-selective peptidomimetic inhibitors of tissue transglutaminase (TG2) were developed through a combination of protein-ligand docking and molecular dynamic techniques. Derivatives of these inhibitors were made with the aim of specific TG2 targeting to the intra- and extracellular space. A cell-permeable fluorescently labeled derivative enabled detection of in situ cellular TG2 activity in human umbilical cord endothelial cells and TG2-transduced NIH3T3 cells, which could be enhanced by treatment of cells with ionomycin. Reaction of TG2 with this fluorescent inhibitor in NIH3T3 cells resulted in loss of binding of TG2 to cell surface syndecan-4 and inhibition of translocation of the enzyme into the extracellular matrix, with a parallel reduction in fibronectin deposition. In human umbilical cord endothelial cells, this same fluorescent inhibitor also demonstrated a reduction in fibronectin deposition, cell motility, and cord formation in Matrigel. Use of the same inhibitor in a mouse model of hypertensive nephrosclerosis showed over a 40% reduction in collagen deposition.
A new, efficient, and catalyst-free microwave-assisted approach for formation of O-tert-butoxy carbonates
K'tir, Hacene,Amira, Aicha,Berredjem, Malika,Aouf, Nour-Eddine
supporting information, p. 851 - 853 (2014/06/23)
A new simple, efficient, greener, and catalyst-free chemoselective protocol for the O-tert-butoxycarbonylation of various structurally diverse hydroxy compounds was carried out with (Boc)2O under microwave radiation. The corresponding O-tertbutoxy carbonates were obtained in good to excellent yields in a short reaction time without any side reactions.
Mixed metal MgO-ZrO2 nanoparticle-catalyzed O-tert-Boc protection of alcohols and phenols under solvent-free conditions
Gawande, Manoj B.,Shelke, Sharad N.,Branco, Paula S.,Rathi, Anuj,Pandey, Rajesh K.
experimental part, p. 395 - 400 (2012/09/25)
An environmentally benign method for O-tert-Boc protection of alcohols and phenols catalyzed by MgO-ZrO2 nanoparticles under solvent-free conditions is described. A variety of phenols, alcohols (aliphatic and aromatic) were converted to corresponding O-tert-Boc products in good to excellent yield (50-95%). The present protocol is expedient, simple, and efficient under solvent-free conditions. The MgO-ZrO2 Nps are easily prepared from inexpensive precursors, and are reusable, recyclable and chemoselective. Copyright 2012 John Wiley & Sons, Ltd. Copyright
An eco-sustainable erbium(iii)-catalyzed method for formation/cleavage of O-tert-butoxy carbonates
Procopio, Antonio,Cravotto, Giancarlo,Oliverio, Manuela,Costanzo, Paola,Nardi, Monica,Paonessa, Rosina
experimental part, p. 436 - 443 (2011/04/17)
A new simple and effective method for the formation/cleavage of O-tert-butoxy carbonates of alcohols and phenols is proposed. Mesoporous silica-supported Er(iii) (ErIII-MCM-41) was used as an efficient and reusable solid catalyst in the solvent-free ultrasound-assisted synthesis of Boc-carbonate derivatives of a wide range of alcohols and phenols. The fast, selective deprotection of Boc-derivatives is achieved with a very low amount of Er(OTf)3 in ethanol under microwave irradiation. Therefore, the entire protection/de-protection process is very attractive, from the point of view of sustainability.
NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 34-35, (2011/10/04)
The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 26, (2011/10/02)
The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
Chemoselective O-tert-butoxycarbonylation of phenols using 6,7-dimethoxyisoquinoline as a novel organocatalyst
Saito, Yukako,Yoshimura, Yuichi,Takahata, Hiroki
experimental part, p. 6915 - 6917 (2011/03/18)
The chemoselective O-tert-butoxycarbonylation of phenols using low levels (5-0.1 mol %) of 6,7-dimeth-oxyisoquinoline as a reusable organocatalyst is described.
