- Functionalization of single-walled carbon nanotubes with (R-)oxycarbonyl nitrenes
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Sidewall functionalization of single-walled carbon nanotubes (SWCNTs) via the addition of (R-)-oxycarbonyl nitrenes allows for the covalent binding of a variety of different groups such as alkyl chains, aromatic groups, dendrimers, crown ethers, and oligoethylene glycol units. Such additions lead to a considerable increase in the solubility in organic solvents such as 1,1,2,2-tetrachloroethane (TCE), dimethyl sulfoxide (DMSO), and 1,2-dichlorobenzene (ODCB). The highest solubilities of 1.2 mg/mL were found for SWCNT adducts with nitrenes containing crown ether of oligoethylene glycol moieties in DMSO and TCE, respectively. The presence of chelating donor groups within the addends allowed for the complexation of Cu2+ and Cd2+. Atomic force microscopy (AFM) and transmission electron microscopy (TEM) revealed that the functionalized tubes form thin bundles with typical diameters of 10 nm. The presence of thin bundles in solution is supported by 1H NMR spectroscopy. The elemental composition of the functionalized SWCNT was determined by X-ray photoelectron spectroscopy (XPS). The use of Raman and electron absorption spectroscopy (UV/Vis-nIR) showed that the electronic properties of the SWCNTs are mostly retained after functionalization, indicating a low degree of addition within this series of SWCNT derivatives.
- Holzinger, Michael,Abraham, Juergen,Whelan, Paul,Graupner, Ralf,Ley, Lothar,Hennrich, Frank,Kappes, Manfred,Hirsch, Andreas
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Read Online
- Solid-phase synthesis of muramyl dipeptide (MDP) derivatives using a multipin method
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Solid-phase synthetic method of muramyl dipeptide derivatives is reported. A diverse library of muramyl dipeptides could be potentially synthesized by acylation, reductive alkylation, sulfonamide formation, urea formation, N-alkylation, amine addition, or component Ugi reactions based on this method for drug screening. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Liu, Gang,Zhang, Shuo-De,Xia, Shu-Quan,Ding, Zhen-Kai
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Read Online
- AZIDE SYNTHESIS WITH STABLE NITROSYL SALTS
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Aryl and acyl hydrazines were converted to azides in excellent yields by an equimolar amount of nitrosyl terafluoroborate or nitrosyl sulfate.
- Pozsgay, Vince,Jennings, Harold J.
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Read Online
- The enantioselective addition of 1-fluoro-1-nitro(phenylsulfonyl)methane to isatin-derived ketimines
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An asymmetric organocatalytic addition of fluorinated phenylsulfonylnitromethane to isatin-derived ketimines was developed. The reaction was efficiently catalyzed by a chiral tertiary amine, cinchonine. This methodology provides a new type of optically active compound with two adjacent quaternary carbon stereocenters in good yield (up to 96%), with moderate diastereoselectivity (up to 5.7:1 dr) and excellent enantioselectivity (up to 98/96% ee).
- Urban,Franc,Hofmanová,Císa?ová,Vesely
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p. 9071 - 9076
(2017/11/14)
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- Cesium Carboxylate-Promoted Iridium Catalyzed C-H Amidation/Cyclization with 2,2,2-Trichloroethoxycarbonyl Azide
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An Ir(III)-catalyzed direct C-H amidation/cyclization of benzamides using 2,2,2-trichloroethoxycarbonyl azide (TrocN3) as the aminocarbonyl source is reported. With the aid of cesium carboxylate, the reactions proceed efficiently and with high regioselectivity, producing various functionalized quinazoline-2,4(1H,3H)-diones, which are important building blocks and key synthetic intermediates for biologically and medicinally important compounds. During the reactions, two new C-N bonds were formed by breaking C-H and N-H bonds sequence.
- Zhang, Tao,Wang, Zhen,Hu, Xuejiao,Yu, Meng,Deng, Tianning,Li, Guigen,Lu, Hongjian
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p. 4898 - 4905
(2016/07/06)
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- Rhodium-Catalyzed N-tert-Butoxycarbonyl (Boc) Amination by Directed C H Bond Activation
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N-tert-Butoxycarbonyl azide (BocN3) was shown to be an efficient and economic source for the directed introduction of N-Boc protected amino groups into the thiophene and benzene nucleus. Yields for the amination of 2-pyridin-2-ylthiophenes (10 examples) were 52–88%. For the amination of the respective benzenes (10 examples) yields between 54% and 99% were recorded with an improved reactivity observed for substrates that bear an electron-withdrawing group. The reaction was applied to short total syntheses of the indoloquinoline alkaloids quindoline and cryptolepine. The facile removal of the Boc protecting group was the key to the success of the syntheses. The scope of the reaction was extended to a C(sp3) H bond amination and to the amination of 2-phenyloxazoline. For the amination of 2-pyridin-2-ylbenzene a kinetic deuterium isotope effect of 2.0 was determined. (Figure presented.) .
- Wippich, Julian,Truchan, Nadina,Bach, Thorsten
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supporting information
p. 2083 - 2087
(2016/07/16)
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- Method for producing hematopoietic stem cells using pyrazole compounds
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An expanding agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful as a therapy for various hematopoietic diseases and useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy is provided. A method of producing hematopoietic stem cells and/or hematopoietic progenitor cells, which comprises expanding hematopoietic stem cells by culturing hematopoietic stem cells ex vivo in the presence of a compound represented by the formula following (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof (wherein R1 to R8 are as defined in the description).
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Page/Page column 169
(2016/01/10)
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- PYRAZOLE COMPOUNDS HAVING THERAPEUTIC EFFECT ON MULTIPLE MYELOMA
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Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6, R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.
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Paragraph 0196; 0197
(2013/10/07)
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- NK1 antagonists
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A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough. wherein the variables are as defined in the specification. A representative compound of the invention is:
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- Synthesis of arylglycines by reaction of diethyl N-Boc-iminomalonate with organomagnesium reagents
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Diethyl N-Boc-iminomalonate (3), prepared on multigram scale, served as a stable and highly reactive electrophilic glycine equivalent which reacted with organomagnesium compounds affording substituted aryl N-Boc-aminomalonates. Subsequent hydrolysis produced arylglycines.
- Calí,Begtrup
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- Stereoselectivity in the Photoinduced Electron Transfer (PET) promoted intramolecular cyclisations of 1-alkenyl-2-silyl-piperidines and -pyrrolidines: Rapid construction of 1-azabicyclo[m.n.0] alkanes and stereoselective synthesis of (±)-isoretronecanol and (±)-epilupinine
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PET promoted cyclisations of 1-alkenyl-2-silyl-pyrrolidines and -piperidines 9a-d to 1-aza-bicyclo[m.n.0]alkanes have been found to be stereoselective. The five-membered ring formation gives predominantly cis products while six-membered rings are trans. Application of such cyclisations to the synthesis of (±)-isoretronecanol 22a, (±)-epilupinine 29 and related alkaloids has been demonstrated. Copyright 1996 by the Royal Society of Chemistry.
- Pandey, Ganesh,Reddy, Gottimukkula Devi,Chakrabarti, Debasish
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p. 219 - 224
(2007/10/03)
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- Platelet activating factor antagonists
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Indole compounds substituted at the 3-position by a 7-carbonyl(pyridin-3-yl)pyrrolo[1,2-c]thiazole, 7-carbonyl(pyridin-3-yl)pyrrolo[1,2-c]oxazole, or 7-carbonyl(pyridin-3-yl)pyrrolo[1,2-c]pyrrole group are potent antagionists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointesinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.
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- Synthesis of Potential Metabolites of 4-Methyl-1-piperazine
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4-Methyl-1-piperazine (1) is an experimental antifilarial drug.In order to investigate its metabolic fate in laboratory animals and also man several potential metabolites, arising from general metabolic conversions of 1, viz.N-oxidation (8), N-demethylation and acetylation (11) and (12), desulphuration (15), nitro group reduction to aryl amino (16) and further acetylation to arylacetamido (17), have been synthesized for identification/quantitation purposes.
- Anjaneyulu B.
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p. 657 - 661
(2007/10/02)
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- Phenyl, trihalomethyl or heteroaryl sulfoxides having a latent allyl group bound to sulfur as enzyme inhibitors
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Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or Kcat type.
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- A NOVEL SYNTHESIS OF (+/-)-3-AMINONOCARDICINIC ACID
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(+/-)-3-Aminonocardicinic acid (3-ANA, 2), which is an important material for the synthesis of nocardicin A (1) and other biologically active analogues, has been synthesized by the application of a new method for the synthesis of α-methylene-β-lactams.
- Chiba, K.,Mori, M.,Ban, Y.
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p. 387 - 392
(2007/10/02)
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- Allylsulfoxide enzyme inhibitors
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Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or Kcat type.
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- Derivatives of L- and DL-4-hydroxyphenylglycine
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L- and DL-isomers of compounds of the formula STR1 and the pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl; R1 is alkynyl, alkenyl or cycloalkyl, each having from three to seven carbon atoms or alkyl having from one to six carbon atoms which may optionally be substituted by one or more groups selected from hydroxy, alkoxy, carboxy, amino, monoalkylamino, dialkylamino, phenyl and phenoxy, any such phenyl or phenoxy being optionally substituted with one or more hydroxy, alkyl or alkoxy groups, said alkyl and alkoxy optional substituents having from one to six carbon atoms; provided that R1 is other than 4-hydroxy-α-carboxybenzyl or 4-methoxy-α-carboxybenzyl. Said compounds are useful in treating diseases and conditions characterized by reduced blood flow, oxygen availability or carbohydrate metabolism in the cardiovascular system. The D-isomers of the compounds of formula (II) are substantially inactive in treating such diseases and conditions.
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- Derivatives of 2-(3-phenyl-2-aminopropionyloxy)-acetic acid
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A compound having the general formula STR1 in which R represents a hydrogen atom or a hydroxyl radical, R1 represents a hydrogen atom or a methyl radical, and R2 represents a phenylethyl radical, a C1 -C16 alkyl radical, or a C6 -C16 monocyclic, polycyclic or alicyclic radical optionally bonded through a methylene radical, and its pharmaceutically acceptable acid addition salts, the formula (I) having the L-configuration when R is OH and when R and R1 are both hydrogen, and having the DL-configuration when R is hydrogen and R1 is methyl. These compounds and salts are useful as medicaments in human and veterinary medicine for cardiovascular and/or neurological treatment.
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- Dihydrocoumarin derivatives
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Process for obtaining 5,6 or 6,7 or 7,8 dihydroxy coumarin or derivatives thereof, which are useful for lower blood pressure and for chemical sympathectomy by oxidizing 2,3 or 3,4 or 4,5 dihydroxyphenyl-propionic acid or derivatives thereof, and novel coumarin derivatives of the process.
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