- Synthesis method of N-BOC-ethylenediamine
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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
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Paragraph 0025-0026
(2021/06/22)
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- MgBr 2 · OEt 2: A Lewis Acid Catalyst for the O - And N -Boc Protection of Phenols and Amines
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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.
- Schechter, Aaron,Goldrich, David,Chapman, Jessica R.,Uberheide, Beatrix M.,Lim, Daniel
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supporting information
p. 653 - 660
(2015/10/29)
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- Development of potent and selective tissue transglutaminase inhibitors: Their effect on TG2 function and application in pathological conditions
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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.
- Badarau, Eduard,Wang, Zhuo,Rathbone, Dan L.,Costanzi, Andrea,Thibault, Thomas,Murdoch, Colin E.,El Alaoui, Said,Bartkeviciute, Milda,Griffin, Martin
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p. 1347 - 1361
(2015/12/26)
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- A new, efficient, and catalyst-free microwave-assisted approach for formation of O-tert-butoxy carbonates
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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.
- K'tir, Hacene,Amira, Aicha,Berredjem, Malika,Aouf, Nour-Eddine
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supporting information
p. 851 - 853
(2014/06/23)
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- Mixed metal MgO-ZrO2 nanoparticle-catalyzed O-tert-Boc protection of alcohols and phenols under solvent-free conditions
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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
- Gawande, Manoj B.,Shelke, Sharad N.,Branco, Paula S.,Rathi, Anuj,Pandey, Rajesh K.
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experimental part
p. 395 - 400
(2012/09/25)
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- An eco-sustainable erbium(iii)-catalyzed method for formation/cleavage of O-tert-butoxy carbonates
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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.
- Procopio, Antonio,Cravotto, Giancarlo,Oliverio, Manuela,Costanzo, Paola,Nardi, Monica,Paonessa, Rosina
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experimental part
p. 436 - 443
(2011/04/17)
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- NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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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.
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Page/Page column 34-35
(2011/10/04)
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- NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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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.
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Page/Page column 26
(2011/10/02)
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- Chemoselective O-tert-butoxycarbonylation of phenols using 6,7-dimethoxyisoquinoline as a novel organocatalyst
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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.
- Saito, Yukako,Yoshimura, Yuichi,Takahata, Hiroki
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experimental part
p. 6915 - 6917
(2011/03/18)
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- Triphenylphosphine as a novel organocatalyst for chemoselective O-tert-butoxycarbonylation of phenols
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A novel organocatalytic procedure for the chemoselective O-tert-butoxycarbonylation of phenols under neutral and neat conditions is described. Georg Thieme Verlag Stuttgart.
- Chebolu, Rajesh,Chankeshwara, Sunay V.,Chakraborti, Asit K.
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p. 1448 - 1454
(2008/12/21)
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- Organocatalytic methods for chemoselective O-tert-butoxycarbonylation of phenols and their regeneration from the O-t-Boc derivatives
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(Chemical Equation Presented) Carbon tetrabromide (CBr4) catalyzes O-tert-butoxycarbonylation of functionalized phenols without any side reactions (bromination, addition of CBr3 to a double bond, and formation of symmetrical diaryl carbonates, cyclic carbonates, or carbonic-carbonic anhydrides). The parent phenols are regenerated from the O-t-Boc derivatives by the catalyst system CBr4-PPh3 without affecting other protecting groups (aryl alkyl ether, alkyl ester, and thioacetal) or competitive side reaction such as bromination, nitrene (from NO2) and α,α-dibromoolefine (with CHO/COMe) formation, and transesterification (with CO2Me/Et) taking place.
- Chankeshwara, Sunay V.,Chebolu, Rajesh,Chakraborti, Asit K.
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scheme or table
p. 8615 - 8618
(2009/04/11)
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- Chemoselective O-tert-butoxycarbonylation of hydroxy compounds using NaLaTiO4 as a heterogeneous and reusable catalyst
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A facile, efficient and chemoselective protocol for O-tert-butoxycarbonylation of various hydroxy compounds has been developed using NaLaTiO4 (layered perovskite) as a novel catalyst. The catalyst showed remarkable activity and reusability affording high yields of the desired products under mild reaction conditions.
- Singh, Savita J.,Jayaram, Radha V.
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p. 4249 - 4251
(2008/09/21)
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- The first simple method of protection of hydroxy compounds as their O-Boc derivatives under Lewis acid catalysis
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The first Lewis acid catalyzed protection of alcohols as Boc derivatives is described. Zinc acetate is a very efficient catalyst for this transformation and the reaction can be applied to primary, secondary and aromatic alcohols, providing the first example of a generally applicable method. Georg Thieme Verlag Stuttgart.
- Bartoli, Giuseppe,Bosco, Marcella,Carlone, Armando,Dalpozzo, Renato,Locatelli, Manuela,Melchiorre, Paolo,Palazzi, Paolo,Sambri, Letizia
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p. 2104 - 2108
(2008/02/05)
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- A novel tert-butoxycarbonylation reagent: 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline (BBDI)
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The use of 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline (BBDI) as a tert-butoxycarbonylation reagent for acidic proton-containing substrates such as phenols, aromatic and aliphatic amines hydrochlorides, and aromatic carboxylic acids in the absence of a base is described. The reactions proceed chemoselectively in high yield under mild conditions.
- Saito, Yukako,Ouchi, Hidekazu,Takahata, Hiroki
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p. 11599 - 11607
(2007/10/03)
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- Synthetic procedures for peptide nucleic acids
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A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
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- Linked peptide nucleic acids
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Novel peptide nucleic acids and novel linked peptide nucleic acids, form triple stranded structures with nucleic acids. The peptide nucleic acids include ligands such as naturally occurring nucleobases attached to the peptide backbone through a suitable linker. Other nucleobases including C-pyrimidines and iso-pyrimidines can be used as the ligands in Hoogsteen strands to increase binding affinity. Two peptide nucleic acid strands are joined together with a linker to form a bis-peptide nucleic acid. The individual strands of the peptide nucleic acids in the bis compounds can be oriented either parallel or antiparallel to each other.
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- Peptide nucleic acids
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Novel peptide nucleic acids and novel linked peptide nucleic acids, form triple stranded structures with nucleic acids. The peptide nucleic acids include ligands such as naturally occurring nucleobases attached to a peptide backbone through a suitable linker. Other nucleobases including C-pyrimidines and iso-pyrimidines can be used as the ligands in Hoogsteen strands to increase binding affinity. Two peptide nucleic acid strands are joined together with a linker to form a bis-peptide nucleic acid. The individual strands of the peptide nucleic acids in the bis compounds can be orientated either parallel or antiparallel to each other.
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- PEPTIDE NUCLEIC ACID CONJUGATES
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A novel class of peptide nucleic acids are described which include a conjugate attached thereto. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
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- 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline: A novel and chemoselective tert-butoxycarbonylation reagent
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(formula presented) The use of 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline (BBDI) as tert-butoxycarbonylation reagent for aromatic and aliphatic amine hydrochlorides and phenols in the absence of a base has been demonstrated. The reactions proceed chemoselectively in high yield under mild conditions.
- Ouchi, Hidekazu,Saito, Yukako,Yamamoto, Yutaka,Takahata, Hiroki
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p. 585 - 587
(2007/10/03)
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- Imidazole and trifluoroethanol as efficient and mild reagents for destruction of excess di-tert-butyl dicarbonate [(BOC)2O]1
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Mild and efficient procedures employing inexpensive reagents (imidazole or trifluoroethanol) for the removal of excess (BOC)2O, usually used during NH or OH protection at room temperature, are described. The use of polymer-based DMAP with or without TFE was also found to be attractive.
- Basel,Hassner
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p. 550 - 552
(2007/10/03)
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- Double-stranded peptide nucleic acids
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A novel class of compounds, known as peptide nucleic acids, form double-stranded structures with one another and with ssDNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
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- Peptide nucleic acids
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A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
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- Structure-activity studies of the binding of modified peptide nucleic acids (PNAs) to DNA
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Peptide nucleic acid (PNA) oligomers where one of the repeating backbone units is extended with a methylene group to either N-(2-aminoethyl)-β-alanine or N-(3-aminopropyl)glycine were prepared. Alternatively, the linker to the nucleobase was extended from
- Hyrup, Birgitte,Egholm, Michael,Nielsen, Peter E.,Wittung, Pernilla,Nordén, Bengt,Buchardf, Ole
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p. 7964 - 7970
(2007/10/02)
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