Abstract: Embodiments of the present disclosure describe a method of synthesizing a glycidyl azide homopolymer comprising contacting a glycidyl azide monomer, an initiator, and a Lewis acid sufficient to form the glycidyl azide homopolymer; wherein the glycidyl azide homopolymer is directly polymerized from the glycidyl azide monomer. Embodiments of the present disclosure further describe a method of making a glycidyl azide polymer comprising contacting one or more of a glycidyl azide monomer, an epoxide monomer, carbon dioxide, an initiator, and a Lewis acid in a reaction medium to form a glycidyl azide polymer.

Abstract: This invention provides metal nanoparticles (e.g., aluminum, chromium, iron and magnesium) having an epoxide-based oligomer coating, compositions thereof, method of making the same, and methods of use thereof, including for energy related applications.

Abstract: Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.

Abstract: The present invention provides a method to label phospholipids in vivo based on the metabolic incorporation of an alkynyl- or azido-labeled metabolic precursor into phospholipids. The resulting phospholipids have alkynyl or azido moieties, which, upon reaction with a labeled azide or alkyne, respectively, form labeled compounds that can be visualized using optical or electron microscopy with high sensitivity and spatial resolution in cells or tissue. The present method provides a valuable tool for imaging phospholipid synthesis, turnover and subcellular localization in cultured cells as well as in animals.

Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).

Abstract: The present disclosure is directed to a reactive ester agent for conjugating a click-reactive group to a carrier molecule or solid support. The reactive ester agent has the general formula IA, wherein the variables R1, R2, R3, Ra and L are described throughout the application.

Abstract: The invention discloses a compound having branching alkyl chains, the method for preparing the same and use thereof in photoelectric devices. By applying the branching alkyl chains as the solubilizing group to the preparation of organic conjugated molecules (for example, organic conjugated polymers), the number of methylenes between the resultant alky side chains and the backbone, i.e., m>1, which can effectively reduce the effect of the alkyl chains on the backbone ?-? stacking, thereby ensuring the solubility of the organic conjugated molecule while greatly increasing the mobility of their carriers. It is suitable for an organic semiconductor material in photoelectric devices such as organic solar cells, organic light emitting diodes and organic field effect transistors, etc.

Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).

Abstract: This invention relates to the synthesis of polymers. More specifically, the present invention relates to the synthesis of heterobifunctional polymers and polymers with narrow and mono-disperse molecular weight distributions, and especially to the application of membranes to the synthesis of these polymers.

Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Abstract: The invention relates to compounds which can be used for purifying peptides produced by solid phase peptide synthesis. In addition, the invention relates to methods for purifying peptides produced by solid phase peptide synthesis using the compounds according to the invention.

Abstract: Novel resorcinol derivatives and methods of preparation and use are presented. These compounds can stimulate angiogenesis as a biological function triggered by the activation of one cannabinoid receptor distinct from CB1 and CB2. Thus, these compounds are specific ligands for one cannabinoid receptor distinct from CB1 and CB2. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.

Abstract: The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples.

Abstract: A new method of ortho-fluorination where an aryl C—H bond is directly replaced by an aryl C-F bond in a palladium-catalyzed reaction is provided. The method includes the ortho-fluorination of a triflamide protected benzylamine, a palladium catalyst, such as Pd(OTf)2, a fluorinating reagent such as N-fluoro-2,4,6-trimethylpyridinium triflate, and a ligand to promote the reaction such as N-methylpyrrolidinone (NMP).

Abstract: The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3? each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.

Abstract: The present invention provides a method to label phospholipids in vivo based on the metabolic incorporation of an alkynyl- or azido-labeled metabolic precursor into phospholipids. The resulting phospholipids have alkynyl or azido moieties, which, upon reaction with a labeled azide or alkyne, respectively, form labeled compounds that can be visualized using optical or electron microscopy with high sensitivity and spatial resolution in cells or tissue. The present method provides a valuable tool for imaging phospholipid synthesis, turnover and subcellular localization in cultured cells as well as in animals.

Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: The graft copolymer comprises a polymerizable monomer (A1) represented by general formula (III) and a polymerizable monomer (B1) containing a pyridyl group, and a ligand can be bonded via the functional group at the terminus of R3a. In the formula, R1a represents a polymerizable group, R2a represents an alkylene group having a carbon number of 2-5, R3a represents an organic group having at a terminus a functional group selected from among an azide group, a phenyl azide group, a carboxyl group, a primary to quaternary amino group, an acetal group, an aldehyde group, a thiol group, a disulfide group, an active ester group, a trialkoxysilyl group, and a polymerizable group, and n represents any integer from 5 to 20,000.

Abstract: The invention provides water-soluble compounds that include a polymer and at least one terminal azide or acetylene moiety. Also provided are highly efficient methods for the selective modification of proteins with PEG derivatives, which involves the selective incorporation of non-genetically encoded amino acids, e.g., those amino acids containing an azide or acetylene moiety, into proteins in response to a selector codon and the subsequent modification of those amino acids with a suitably reactive PEG derivative.

Abstract: Novel glycolipid derivatives, where the substituent of the sphingosine base part is a short carbon chain alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group and efficient synthetic methods for practical mass production of the same and intermediates useful for the synthesis of these compounds. Glycolipids having the formula (I): where R3 indicates a substituted or unsubstituted C1 to C7 linear alkyl group, substituted or unsubstituted cycloalkyl group, substituted or unsubstituted aryl group, or substituted or unsubstituted aralkyl group and R8 indicates a substituted or unsubstituted C1 to C35 alkyl group, substituted or unsubstituted aryl group or substituted or unsubstituted aralkyl group are chemically synthesized.

Abstract: A method for preparing saturated partially fluorinated alkoxy carboxylic acids or salts thereof by treating a compound: (II), where Rf represents a fluorinated, linear or branched alkyl residue interruptible by one or more oxygen atoms, n is 0 or 1, with a Z-anion in a reaction medium comprising water and an organic solvent, where the Z-anion is selected from CN—, SCN— and OCN— or combinations thereof. A method of making partially fluorinated ethers of the general formula (I) wherein Rf is defined as above, n is 0 or 1, and Z is nitrile (—CN), azide (—N3), thiocyanate (—SCN) or cyanate (—OCN) group, said method comprising treating a fluorinated olefin of the general formula (II) wherein the Z-anion is CN—, OCN—, SCN— or N3?. A compound of the general formula (I) as previously described where Z is selected from SCN, OCN and N3.

Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Abstract: Aspects of the present invention are directed to novel methods for making discrete polyethylene compounds selectively and specifically to a predetermined number of ethylene oxide units. Methods which can be used to build up larger dPEG compounds (a) containing a wider range of utility to make useful homo- and heterofunctional and branched species, and (b) under reaction configurations and conditions that are milder, more efficient, more diverse in terms of incorporating useful functionality, more controllable, and more versatile then any conventional method reported in the art to date. In addition, the embodiments of the invention allow for processes that allow for significantly improving the ability to purify the intermediates or final product mixtures, making these methods useful for commerial manufacturing dPEGs. Protecting groups and functional groups can be designed to make purification at large scale a practical reality.

Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Abstract: The invention relates to methods and apparatus for purifying a radiolabelled compound. The method comprises (i) passing a crude reaction mixture comprising the desired radiolabelled compound and one or more contaminants in a solvent through a narrow bore vessel at elevated temperature such that the organic solvent and either the radiolabelled compound or one or more contaminants is vaporised forming a vaporised component, and (ii) collecting the resulting vaporised component by condensing into a collection vessel.

Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N3 (II) or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Abstract: The high efficiency and fidelity of click chemistry permits a large number of diverse dendrimers encompassing a wide variety of functionalities at the chain ends, repeat units, and/or core to be prepared. Almost quantitative yields were obtained during the synthesis. In some cases, filtration or solvent extraction was the only method required for purification. These features represent a significant advancement in dendrimer chemistry and demonstrate an evolving synergy between organic chemistry and functional materials.

Abstract: A composition includes a Group (VIII) transition metal, an anionic ligand bonded to the metal, a neutral electron donor ligand bonded to the metal, and an alkylidene group bonded to the metal. The alkylidene group includes a cycloaliphatic radical substituted with an ionic group. An associated method is also provided.

Abstract: The present invention relates to 5-azido levulinic acid, a process for its preparation, its use. Using 5-azido levulinic acid as starting material for the synthesis of 5-amino levulinic acid hydrochloride it is possible to obtain the latter in good yield an in pharmaceutical acceptable quality. 5-Azido levuliniv acid is synthesized in that methyl 5-bromo levulinate and/or methyl 5-chloro levulinate is converted with aqueous hydrochloric acid and as a result of an incomplete bromine/chlorine exchange at the C-5-postion a mixture of 5-chloro levulinic acid and 5-bromo levulinic acid is obtained, and the obtained 5-chloro levulinic acid, a mixture of 5-chloro levulinic acid and 5-bromo levulinic acid and the pure 5-bromo levulinic acid is transferred into 5-azido levulinic acid by conversion with a nucleophilic azide.

Abstract: The invention relates to a novel polyazido compound: 2,2-dinitro-1,3-diazidopropane.

Abstract: The invention provides methods and compositions for azide tagging of biomolecules. In one embodiment of the invention, proteins are tagged by metabolic incorporation of prenylated azido-analog substrates. Examples of such analogs are azido farnesyl diphosphate and azido farnesyl alcohol. The azido moiety in the resulting modified proteins provides an affinity tag, which can be chemoselectively captured by an azide-specific conjugation reaction, such as the Staudinger reaction, using a phosphine capture reagent. When the capture agent is biotinylated, the resulting conjugates can be detected and affinity-purified by streptavidin-linked- HRP and streptavidin-conjugated agarose beads, respectively. The invention allows detection and isolation of proteins with high yield, high specificity, and low contamination without harsh treatment of proteins.

Abstract: A method for preparing organic products from aqueous solutions, such as waste or byproduct liquid streams and waste or byproduct gas or vapor streams, uses phase transfer catalysis to transfer a chemical species in low concentration from the aqueous solution to the organic phase or the aqueous-organic interface. The system has little or no organic solvent, and the organic phase contains an electrophile which participates in the reaction. In one embodiment, the aqueous solution is contacted with the electrophile and a phase transfer catalyst and, optionally, a pH adjusting agent in the event that the chemical species in the aqueous solution is not sufficiently ionized to react with the electrophile, and optionally an organic solvent. A method for continuously converting a chemical species involves this contacting step, separating the phases, then dividing the organic phase into the product, the phase transfer catalyst, and the optional organic solvent.

Abstract: This invention relates to a series of novel compounds having the general structures A and B: including 2-azido-2-azidomethyl-1,3-diazidopropane (1), 2-azidomethyl-2-hydroxy-1,3-diazidopropane (2), 2-azidomethyl-2-nitrato-1,3-diazidopropane (3), 2-azidomethyl-2-nitro-1,3-diazidopropane (4), 2,2-dinitro-1,3-diazidopropane (5), methallyidiazide (6), a dimer of methallyidiazide (6), comprising 3a,8a-Bis-azidomethyl-3a,4,8a,9-tetrahydro-3H,8H-bis[1,2,3]triazolo[1,5-a;1?,5?-d]pyrazine (6-Dimer), 1,3-diazidoacetone (7), and 2-Oximido-1,3-diazidopropane (8). Also shown are reaction intermediates of these compounds, including 2,2-bis(chloromethyl)oxirane (9), and 2,2-bis(azidomethyl)oxirane (10).

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: The present invention provides compounds of formula Ia and Ib or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from disease-causing microorganisms, especially influenza neuraminidase, pharmaceutical formulations containing same, processes and intermediates for preparing said compounds, as well as methods of using said compounds, including preventing and treating diseases caused by microorganisms having said neuraminidase enzyme.

Abstract: The invention provides a novel compound 4-(p-methoxy-phenyl)-2-aminobutane exhibiting growth inhibition and antifeedant activity and represented by the structural formula. C11H17ON=4-(p-methoxy phenyl)-2-amino butane and an insecticidal composition comprising an effective amount of the novel compound and appropriate adjuvant.

Abstract: The invention relates to compounds with the general formula Y1—A1—M1—A2—Y2 wherein Y1 and Y2 are different from each other and Y1 is an acrylate or methacrylate residue and Y2 is a vinyl ether, epoxy, or azide residue, A1 and A2 are identical or different residues with the general formula CnH2n in which n is a whole number from 0 to 20 and one or more methylene groups can be replaced by oxygen atoms, and M1 has the general formula —R1—X1—R2—X2—R3—X3—R4— wherein R1, R2, R3, and R4 are identical or different doubly bonded residues from the group —O—, —COO—, —CONH—, —CO—, —S—, —C≡C—, —CH═CH—, —CH═N—, —CH2—, —N═N—, and —N═N(O)—, and R2—X2—R3 can also be a C—C bond, and X1, X2, and X3 are identical or different residues from the group 1,4-phenylene, 1,4-cyclohexylen

Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.

Abstract: 15-HETE derivatives with enhanced metabolic stability and methods of their use for treating dry eye are disclosed.

Abstract: The invention relates to compounds with the general formula Y1—A1—M1—A2—Y2 wherein Y1 and Y2 are different from each other and Y1 is an acrylate or methacrylate residue and Y2 is a vinyl ether, epoxy, or azide residue, A1 and A2 are identical or different residues with the general formula CnH2n in which n is a whole number from 0 to 20 and one or more methylene groups can be replaced by oxygen atoms, and M1 has the general formula —R1—X1—R2—X2—R3—X3—R4— wherein R1, R2, R3, and R4 are identical or different doubly bonded residues from the group —O—, —COO—, —CONH—, —CO—, —S—, —C≡C—, —CH═CH—, —CH═N—, —CH2—, —N═N—, and —N═N(O)—, and R2—X2—R3 can also be a C—C bond, and X1, X2, and X3 are identical or different residues from the group 1,4-phenylene, 1,4-cyclohexylen

Abstract: A process for the addition of an azide function to an organic compound in which process a mixture is prepared by adding an epoxide-derivative of the organic compound and an alkali metal azide salt to a solvent is described. The mixture is heated to a reaction temperature at which the epoxide-derivative and the azide can react to form an azide derivative of the organic compound. An amount, near equimolar to the epoxide derivative, of a (1-6C)alkyl-(2-4C)carboxylic acid ester having a boiling point above the reaction temperature is added to the mixture before and/or during the reaction.

Abstract: Midodrine hydrochloride, ±1-(2′,5′-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone.

Abstract: A process for the preparation of optically active cyclohexylphenylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.

Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.

Abstract: This invention provides an imageable element comprising a substrate having on at least one major surface thereof a layer of energy-sensitive material that is capable of being developed to form a relief image upon exposure to electromagnetic radiation having a wavelength in the ultraviolet-visible-infrared range (i.e., a wavelength ranging from 150 to 1500 nm). This invention also provides methods for imaging the imageable elements of this invention. The energy-sensitive materials suitable for this invention comprise polymers containing azido groups.

Abstract: The present invention relates to novel 1.alpha.-hydroxy vitamin D derivatives in which the 17-position side chain carries an azide or optionally substituted 1,2,3-triazole group, including compounds of general formula (I) where R.sup.1 represents a methyl group having .alpha.- or .beta.-configuration; W represents a valence bond or a C.sub.1-5 alkylene group; X represents azide or an optionally substituted triazole group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcaemic effect.

Abstract: A process for the preparation of azide derivatives useful as drugs, perfumes or intermediates of dyes by reacting an alcohol derivative with di-p-nitrophenyl phosphorazidate in the presence of 1,8-diazabicyclo[5.4.0]-7-undecene.

Abstract: 1-substituted, 2-substituted 1H-imidazo[4,5-c]-quinolin-4-amines are disclosed. These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract: Synthesis of a vinyl terminated polymer by reacting a cationically polymeable monomer in the form of a cyclic ether with an acid chloride in a suitable solvent and in the presence of a Lewis acid. The vinyl-terminated polymers can be polymerized with other appropriate monomers resulting in thermoplastic elastomers having suitable properties for use as binders for explosives and propellants.

Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.