Showing papers on "Derivative (chemistry) published in 2005"
TL;DR: Alpha-amino phosphonates were obtained with good to high enantioselectivities in hydrophosphonylation of aldimines with diisopropyl phosphite at room temperature.
264 citations
TL;DR: A review of reactions scaled in the GMP facilities at the Pfizer-Groton site was undertaken as mentioned in this paper, where reactions were categorized into one of seven categories: carbon−carbon bond formation, carboxylic acid derivative interconversion, carbon−nitrogen bond formation and carbon−oxygen bond formation.
263 citations
TL;DR: In vitro anticancer studies on MCF-7 human breast cancer cells reveal that the semicarbazone derivative along with its nickel complex is more active in the inhibition of cell proliferation than the thiosemicarbazones analogue.
180 citations
Patent•
04 Apr 2005TL;DR: In this article, an organic electroluminescent (OEL) compound was used as a host material for fluorescent and phosphorescent dopants of all colors including red, green, blue, white, etc.
Abstract: The present invention relates to an organic electroluminescent (OEL) compound that comprises at least one fluorene derivative and at least one carbazole derivative. The compound has good electrical properties, light emitting properties and charge transport ability, and thus is suitable as a host material suitable for fluorescent and phosphorescent dopants of all colors including red, green, blue, white, etc., and as a charge transport material. An OEL display device that uses an organic layer that includes the OEL compound has a high efficiency, a low voltage, a high luminance, and a long lifespan because it has superior current density.
164 citations
TL;DR: Self-assembly of a fullerene derivative with long alkyl chains in different solvents results in the formation of hierarchically-ordered supramolecular assemblies with well-defined 1, 2 and 3D architectures such as vesicles, fibers, discs and cones, whose fundamental structural sub-unit consists of bilayers.
142 citations
118 citations
TL;DR: The Fmoc solid-phase synthesis of peptide thioesters based on the alkylation of the safety-catch sulfonamide linker with a protected 2-mercaptoethanol derivative is described.
112 citations
TL;DR: Pentakis(1,4-benzodithiino)corannulenes in CS2 formed the strongest 1:1 complexes with C60 and C70 of any corannulene derivative yet reported, while the 1,3,5,7,9-pentakis(propylthio)cor Annulene (4b) and unsubstituted corannULene showed no evidence for complexation with either C60 or C70 inCS2.
Abstract: Pentakis(1,4-benzodithiino)corannulene (6) in CS2 formed the strongest 1:1 complexes with C60 and C70 of any corannulene derivative yet reported. The 1,3,5,7,9-pentakis(propylthio)corannulene (4b) formed weaker 1:1 complexes with C60 and C70 in CS2, whereas the decakis(propylthio)corannulene (5b) and unsubstituted corannulene (1) showed no evidence for complexation with either C60 or C70 in CS2.
96 citations
TL;DR: Copper and CuFe Prussian Blue nanoparticles have been prepared by using a Cu(II)-loaded apoferritin as a chemically and spatially confined environment for their construction.
Abstract: Copper and CuFe Prussian Blue nanoparticles have been prepared by using a CuII-loaded apoferritin as a chemically and spatially confined environment for their construction.
93 citations
TL;DR: An isomeric mixture of a tris(pentafluorobenzyl ester) derivative of hexaazatrinaphthylene forms stable amorphous films with an effective charge-carrier mobility of 0.02 cm2/Vs, while the pure 2,8,15-isomer exhibits widely differing morphologies and carrier mobilities.
Abstract: An isomeric mixture of a tris(pentafluorobenzyl ester) derivative of hexaazatrinaphthylene forms stable amorphous films with an effective charge-carrier mobility of 0.02 cm2/Vs, while the pure 2,8,15-isomer exhibits widely differing morphologies and carrier mobilities (0.001−0.07 cm2/Vs), depending critically on the processing conditions.
91 citations
TL;DR: Systematic studies on the DNA binding of a new anthracene derivative, carrying a 1,8-octyldiamine side chain, showed that the side chain enhances the binding constant by a factor of approximately 35 when compared to thebinding of a probe lacking the long side chain.
Abstract: Systematic studies on the DNA binding of a new anthracene derivative, carrying a 1,8-octyldiamine side chain, were carried out. Calorimetric, spectroscopic, and helix melting studies show that the ...
TL;DR: A novel racemization catalyst was synthesized for the dynamic kinetic resolution (DKR) of alcohols with a lipase at room temperature in the air and a polymer-supported derivative was also synthesized and tested as a recyclable catalyst for the aerobic DKR ofalcohols.
TL;DR: A chromatography-free preparation of an iodolactone, by using acryloyl chloride as the dienophile in the Diels-Alder reaction of furan, and the lipase-mediated kinetic resolution of a cyclohexenol derivative have been developed, suitable for large-scale preparation.
Abstract: Full details of two versions of the total synthesis of epoxyquinols A, B, and C and epoxytwinol A (RKB-3564D) are described. In the first-generation synthesis, the HfCl(4)-mediated diastereoselective Diels-Alder reaction of furan with Corey's chiral auxiliary has been developed. In the second-generation synthesis, a chromatography-free preparation of an iodolactone, by using acryloyl chloride as the dienophile in the Diels-Alder reaction of furan, and the lipase-mediated kinetic resolution of a cyclohexenol derivative have been developed. This second-generation synthesis is suitable for large-scale preparation. A biomimetic cascade reaction involving oxidation, 6pi-electrocyclization, and then Diels-Alder dimerization is the key reaction in the formation of the complex heptacyclic structure of epoxyquinols A, B, and C. Epoxytwinol A is synthesized by the cascade reaction composed of oxidation, 6pi-electrocyclization, and formal [4 + 4] cycloaddition reactions. A 2H-pyran, generated by oxidation/6pi-electrocyclization, acts as a good diene, reacting with several dienophiles to afford polycyclic compounds in one step. An azapentacyclic compound is synthesized by a similar cascade reaction composed of the four successive steps: oxidation, imine formation, 6pi-azaelectrocyclization, and Diels-Alder dimerization.
Patent•
23 May 2005TL;DR: In this paper, a monoreactive tetra-alkyl DTPA derivative is manufactured using a metal ion as a catalytic catalyst, where the DTPA is first prepared and then processes a regioselective hydrolysis over the penta-alky DTPA.
Abstract: The present invention at first prepares a penta-alkyl DTPA and then processes a regioselective hydrolysis over the penta-alkyl DTPA while using a metal ion as a catalyst to obtain a tetra-alkyl DTPA, where, by the above two steps, a monoreactive DTPA derivative is manufactured.
TL;DR: The intramolecular photocycloaddition of a 1-cyanonaphthalene derivative in microreactors made of poly(dimethylsiloxane) (PDMS) was examined.
Abstract: The intramolecular photocycloaddition of a 1-cyanonaphthalene derivative in microreactors made of poly(dimethylsiloxane) (PDMS) was examined. By using the microreactors and flow system, both the ef...
TL;DR: In this paper, the reactivity of 2-phosphine sulfide substituted phosphinines toward alkynes was examined, and it was shown that formation of 1-phphosphabarrelenes is thermodynamically favored when dimethyl acetylenedicarboxylate is available.
TL;DR: The diastereoselective oxidative cyclization of a dihydrooroidin derivative is reported and the thioimidate product formed by application of a new variant of the Pummerer reaction serves as a precursor to dibromophakellstatin.
Patent•
25 Feb 2005TL;DR: A compound represented by the following general formula, a salt thereof, or a hydrate of either, is a compound with excellent inhibitory activity against a hepatocyte growth factor receptor (HGFR) and have antitumor activity, angiogenesis inhibitory activities, or cancer metastasis inhibitory action as discussed by the authors.
Abstract: A compound represented by the following general formula, a salt thereof, or a hydrate of either. They have excellent inhibitory activity against a hepatocyte growth factor receptor (HGFR) and have antitumor activity, angiogenesis inhibitory activity, or cancer metastasis inhibitory activity. (In the formula, R1 means C1-6 alkyl, etc.; R2 and R3 each means hydrogen; R4, R5, R6, and R7 are the same or different and each means hydrogen, halogeno, C1-6 alkyl, etc.; R8 means hydrogen, etc.; R9 means C1-6 alkyl, etc.; V1 means oxygen, etc.; V2 means oxygen or sulfur; W means -NH-, etc.; X means -CH=, nitrogen, etc.; and Y means oxygen, etc.)
TL;DR: In this paper, a cationic beta-glucan derivative of oats was extracted from oats and was subjected to reductive amination, producing a Cationic Beta-Glucan derivatives of which physiological properties were characterized.
Abstract: beta-Glucan extracted from oats was subjected to reductive amination, producing a cationic beta-glucan derivative of which physiological properties were characterized. The degree of substitution was obtained from elemental analysis, which was 0.48. In addition, the distribution of amino groups in the beta-glucan derivative was investigated by FT-IR analysis. In vitro bile acid binding capacity of the aminated beta-glucan was examined, showing significantly higher bile acid binding activity than native beta-glucan. Moreover, the beta-glucan derivative showed pronounced antimicrobial effects against Escherichia coli and Bacillus subtilis, and ACE (angiotensin-converting enzyme) inhibition activities which were dependent on its concentration. Furthermore, bronchoalveolar lavage (BAL) experiments demonstrated that the beta-glucan derivative stimulated the synthesis of nitric oxide. The improved functionalities of the derivative could be explained by its polycationic characteristics.
Patent•
03 Aug 2005
TL;DR: In this article, a compound represented by the formula (I) below and an agriculturally and horticulturally acceptable acid addition salt thereof have excellent insecticidal activity and can be used as an insecticide for agricultural and Horticultural use.
Abstract: Disclosed is a compound having excellent insecticidal activity and usable as an insecticide for agricultural and horticultural use. A compound represented by the formula (I) below and an agriculturally and horticulturally acceptable acid addition salt thereof have excellent insecticidal activity and can be used as an insecticide for agricultural and horticultural use.
TL;DR: A supramolecular poly[3]pseudorotaxane was prepared by self-assembly of a homoditopic cylindrical bis(crown ether) host and a bisparaquat derivative in solution by host-guest complexation.
TL;DR: Articles about the development of derivative spectrophotometric methods and analytical applications of derivative Spectrophotometry (DS) published in the last nine years (since 1994) are reviewed.
Abstract: Articles about the development of derivative spectrophotometric methods and analytical applications of derivative spectrophotometry (DS) published in the last nine years (since 1994) are reviewed.
TL;DR: A new family of bifunctional agents that combine two modalities into a single cost-effective "see and treat" approach is described, namely, a single agent that can be used for contrast agent-enhanced MR imaging followed by targeted photodynamic therapy.
TL;DR: Total syntheses of (+)-cytisine, (-)-kuraramine, (--isokuraramines, and (-)-jussiaeiine A were achieved via a samarium diiodide-promoted reductive deamination reaction, followed by simultaneous recyclization of a proline derivative to give the corresponding delta-lactam derivative, as a key step.
Abstract: Total syntheses of (+)-cytisine, (−)-kuraramine, (−)-isokuraramine, and (−)-jussiaeiine A were achieved via a samarium diiodide-promoted reductive deamination reaction, followed by simultaneous recyclization of a proline derivative to give the corresponding δ-lactam derivative, as a key step.
Patent•
26 Jul 2005
TL;DR: A glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia such as diabetes, complications of diabetes, and obesity.
Abstract: A glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): (wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl), a prodrug of the compound,or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.
TL;DR: Two new naphthoquinone macrolides were isolated from the fermentation broth of Streptomyces hygroscopicus and the structure of hygrocin B was determined by combined chemical and spectroscopic methods.
Abstract: Two new naphthoquinone macrolides, hygrocins A (1) and B (2), were isolated from the fermentation broth of Streptomyces hygroscopicus. Hygrocin A is not stable due to the presence of an active methylene group (C-22), which undergoes intramolecular aldol condensation with the quinone ring to yield a γ-lactam derivative, 6. Its structural elucidation was achieved by chemical conversion to 3, an unusual diazomethane derivative, and confirmed by its alkaline hydrolysis product 4, hydrogenation derivative 5, and “degradation” product 6. The structure of hygrocin B was determined by combined chemical and spectroscopic methods.
TL;DR: Starting from L-serine, a stereoselective synthesis of pachastrissamine, a structurally novel anhydrosphingosine derivative, is reported in this Letter.
Patent•
14 Jan 2005TL;DR: In this article, the authors presented a cathode having a complex between the surface of a cathodes active material and an aliphatic nitrile compound, as well as an electrochemical device comprising the cathode.
Abstract: The present invention provides a cathode having a complex between the surface of a cathode active material and an aliphatic nitrile compound, as Well as an electrochemical device comprising the cathode. Also, the comprising : (1) a cathode having a complex between the surface of cathode active material and an aliphatic nitrile compound ; (2) an anode having a passivation layer formed by a compound selected from the group consisting of vinylene carbonate, its derivative and an ether compound ; and (3) an electrolyte solution containing a lithium salt and a solvent.
TL;DR: 3,4-Bis(3-nitrofurazan-4-yl)furoxan has been synthesized bynitration of C,N-bis(trimethylsilyl)derivative of 3-amino-4methylfurazan with nitrogenoxides as discussed by the authors.