Abstract: A method of forming an azido energetic alcohol includes converting an energetic diol to a cyclic sulfite, oxidizing the cyclic sulfite to a cyclic sulfate, and opening the cyclic sulfate. The cyclic sulfate is opened, followed by hydrolysis, to form an azido energetic alcohol.

Abstract: The present invention is directed towards proposing ligands of formula: and is also directed towards a substrate at the surface of which is immobilized at least one unit of formula:

Abstract: Provided are saturated partially fluorinated alkoxy carboxylic acids or salts thereof and methods of preparation.

Abstract: Provided are saturated partially fluorinated alkoxy carboxylic acids or salts thereof and methods of preparation.

Abstract: Novel PEG multifunctional derivatives. A PEG backbone molecule is covalently attached with at least three different functional groups, either on the same branch arm or on different branch arms.

Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.

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 provides compositions and methods for producing translational components that expand the number of genetically encoded amino acids in eukaryotic cells. The components include orthogonal tRNAs, orthogonal aminoacyl-tRNA synthetases, pairs of tRNAs/synthetases and unnatural amino acids. Proteins and methods of producing proteins with unnatural amino acids in eukaryotic cells are also provided.

Abstract: A method of forming an azido energetic alcohol includes converting an energetic diol to a cyclic sulfite, oxidizing the cyclic sulfite to a cyclic sulfate, and opening the cyclic sulfate. The cyclic sulfate is opened, followed by hydrolysis, to form an azido energetic alcohol.

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 present invention is directed towards proposing ligands of formula: and is also directed towards a substrate at the surface of which is immobilized at least one unit of formula:

Abstract: The invention provides a method of preparing the stereoisomers of 1,11-diamino-6-aza-undecane-2,4,8,10-tetraol.

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: A process of synthesizing hyperbranched polytriazoles, linear and hyperbranched poly(aroyltriazoles) by Huisgen 1,3-dipolar cycloaddition. The polytriazoles were prepared by A2+B3 method to avoid self-polymerization during monomer preparation and storage. The polymers are light emissive and can be crosslinked to generate well-resolution photopatterns upon UV irradiation. White light emission patterns were observed with fluorescence microscopy. The high molecular weight poly(aroyltriazoles) (up to 26000 Da) are prepared in high yields (up to 92.0%) and with high regioselectivity (the ratio of 1,4- and 1,5-disubstituted 1,2,3-triazole is equal or larger than 9:1). The polycyclomerization is not moisture or oxygen sensitive and therefore, no special precautions are necessary before and during the reaction. All the polymers are processible, easily film-forming, and curable into thermosets by heat or irradiation. The hyperbranched polymers can act as fluorescent adhesive materials with large tensile strength.

Abstract: The present invention concerns methods of synthesis of trans-tert-butyl-2-aminocylcopentylcarbamate comprising contacting 6-tosyl-6-azabicyclo[3.1.0]hexane with TMSN3 and TBAF to produce 2-azido-N-tosylcyclopentananiine; reducing the 2-azido-N-tosylcyclopentanamine to produce 2-amino-N-tosylcyclopentanamine; contacting the 2-amino-N-tosylcyclopentanamine with di-tert/-butyl dicarbonate to produce tert-butyl-2-(tosylamino)cyclopentylcarbamate; and detosylation of tert-butyl O(tosylamino) cyclopentylcarbamate to produce trans-tert-butyl-2-aminocyclopentylcarbamate. The invention also concerns PNAs comprising residues of the monomers of the invention in the backbone and uses of such PNAs. The PNAs of the invention can be used to detect DNAs of infectious agents or to suppress expression of protein associated with cancer.

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 process for enantioselectively preparing 3-azidocarboxylic acid derivatives comprises reacting 3-sulfonatocarboxylic acid derivatives with an alkali metal azide in a solvent selected from the group comprising certain carboxamides; a solvent mixture which comprises such carboxamides; a solvent mixture of water and a solvent miscible homogeneously with water; water with the proviso that the addition of a phase transfer catalyst is not used in the reaction in water; and DMSO. The resulting products are optionally reduced to 3-aminocarboxylic acid derivatives.

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

Abstract: Compounds of formula (XII), are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is reacted with an amine to form a carboxamide, the halogen is replaced with azide, if necessary after the introduction of a hydroxy protecting group, the resulting azide is converted to a lactone, the lactone is amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I) or a salt thereof.

Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: 1

Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

Abstract: The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated diseases, such as fungal infections.

Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

Abstract: The present invention relates to the compound of formulae ##STR1## and to a process for the manufacture of compounds of the general formula ##STR2## which are ligands for the metabotropic glutamate receptors of group II, whereinT is tritium;R.sup.1 is hydroxy, lower alkoxy, lower alkenyloxy, benzyloxy, hydrogen, deuterium or tritium;R.sup.11 is hydrogen, deuterium or tritium, hydroxy or amino, andR.sup.2 is hydrogen or tritium, orR.sup.1 and R.sup.2 form a bond.

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: The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C.sub.20 H.sub.32 O.sub.3. The present invention also provides a purified retinoid compound having the structure: ##STR1## wherein the configuration of the C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively.

Abstract: The present invention relates generally to methods of diagnosis, evaluation and treatment of coronary artery disease in mammals using substituted catecholamines and compounds therefore. It also relates to the preparation, use and administration of these compounds which are useful in the diagnosis, evaluation and treatment of coronary artery disease by means of a feedback controlled drug delivery system that delivers exercise simulating agents which are capable of eliciting acute responses similar to those elicited by aerobic exercise.

Abstract: A process of making certain compounds using a phase transfer catalyst that permits the recovery and recycle of the phase transfer catalyst.

Abstract: A normally liquid, non-detonable product having less than about 45.7 weight percent nitrogen comprising polymer which can be represented by the general formula:R(G).sub.n R.sup.1where, in the above formula,n is a number between 2 and 18;G is an azidomethyloxyethylene moiety;R is a monovalent residue of an organic initiator compound or a monovalent alkyl radical, R is essentially free of isocyanate-reactive moieties and may be substituted with non-interfering atoms or moleties and it cannot be substituted with energetic nitrogen-containing moieties other than azido moleties;R.sup.1 is a monovalent alkoxy radical, oxyaryl radical or combinations thereof, or R.sup.1 is an azido moiety, R.sup.1 is essentially free of isocyanate-reactive atoms or moieties and it may be substituted with non-interferring atoms or moieties and it cannot be substituted with energetic nitrogen-containing moleties other than azido moieties; orR and R.sup.1, taken together, are a carbon-oxygen bond when said polymer is a cyclic compound.

Abstract: Novel multi-azido formals, acetals and ketals are disclosed, having the following generic formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently selected from H, CH.sub.3, and CH.sub.2 N.sub.3, and methods of preparation of these compounds.

Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

Abstract: A process of making poly(glycidyl azide) and 3,6 -dioxadecyl thiocyanate using a phase transfer catalyst that permits the recovery and recycle of the phase transfer catalyst.

Abstract: Glycidyl azide polymers, which are used as binders in composite explosive and propellant compositions, include hydroxyl groups which react with the isocyanate curing agent normally used in such compositions. Since the functionality of available linear glycidyl azide polymers is less than two, triols and/or triisocyanates are needed to crosslink the chains to form a matrix. A glycidyl azide polymer with increased functionality (higher than two) and reactivity obviates the need for triols and triisocyanates in the compositions. Moreover, a glycidyl azide polymer with primary hydroxyl groups would give faster curing reactions at lower temperatures without gassing problems, eliminating the need for a catalyst. Examples of glycidyl azide polymer having increased functionality have one of the formulae: ##STR1## wherein R is ##STR2## wherein m and n are different from zero, and m+n is 4 to 60.

Abstract: A process for obtaining a hydroxy-ended glycidyl azide polymer (GAP). The process consists in reacting polyepichlorohydrin (PECH) with a metallic azide in the presence of an organic solvent having a parameter of solubility comprised between 21 and 23.5 (MPa).sup.1/2 such as DMA or NMP. The use of any of the solvents mentioned sharply reduces the reaction time needed for substituting azide groups for the chlorine present in the PECH. Said reaction times can be less than 4 hours when NMP is used or less than 6 hours when DMA is used. The GAP thus obtained having a functionality equal to or above 2 can be used as energetic bonding agent in the formulation of solid propellants for rockets.

Abstract: This invention relates to the production of hydroxy-terminated polymers in the 2,000-20,000 MW range suitable for use as prepolymers in curing reactions with isocyanates to produce elastomers. The process involves the continuous addition over periods of 25-50 hours of an oxirane (monoepoxide) or a mixture of an oxirane and an oxetane to a reaction mixture, consisting of stoichiometric excesses of oxonium ion-forming catalyst such as BF.sub.3 -etherate and a diol initiator dissolved in an inert solvent. Under these conditions, chain extension of the diol occurs and the formation of cyclic oligomers and other impurities is minimised. The mole ratio of the initiator to catalyst is maintained at above 10:1 to suppress the formation of cationic terminal species on the growing polymer chain.

Abstract: Glycidyl azide polymers, which are used as binders in composite explosive and propellant compositions, include hydroxyl groups which react with the isocyanate curing agent normally used in such compositions. Since the functionality of available linear glycidyl azide polymers is less than two, triols and/or triisocyanates are needed to crosslink the chains to form a matrix. A glycidyl azide polymer with increased functionality (higher than two) and reactivity obviates the need for triols and triisocyanates in the compositions. Moreover, a glycidyl azide polymer with primary hydroxyl groups would give faster curing reactions at lower temperatures without gassing problems, eliminating the need for a catalyst. Examples of glycidyl azide polymer having increased functionality have one of the formulae: ##STR1## wherein R is ##STR2## wherein m and n are different from zero, and m+n is 4 to 60.

Abstract: Novel multi-azido formals, acetals and ketals are disclosed, having the following generic formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently selected from H, CH.sub.3, and CH.sub.2 N.sub.3, and methods of preparation of these compounds.

Abstract: The invention disclosed relates to novel branched chain hydroxy-terminated aliphatic polyether copolymers containing glycidyl azide and an additional substituent selected from the group consisting of alkylene oxide, styrene azide oxide and glycidyl units, and a single step method for the manufacture thereof which involves reacting a solid rubbery material selected from epichlorohydrin/alkylene oxide copolymer (PEEC) and polyepichlorohydrin homopolymer (PECH) with various epoxide monomers. The novel polyether copolymers are useful as energetic binders in explosive and solid rocket propellant compositions.

Abstract: Epichlorohydrin is polymerized with an active hydrogen-containing initiator and the resulting secondary hydroxyl-containing polyepichlorohydrin is further reacted to produce a hydroxyl-terminated polyepichlorohydrin product having chains terminating in a primary hydroxyl group, said polyepichlorohydrin product being reactable with an inorganic azide to produce a poly(glycidyl azide) product useful as a binder for solid rocket propellants.

Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

Abstract: Glycidyl azide polymer is a hydroxy-terminated aliphatic polyether containing alkyl azide groups. Such a polymer could be used as a plasticizer in composite explosives, gun and rocket propellants. However, the hydroxyl groups of the polymer react with the isocyanate of the curing agent, thereby eliminating any possible plasticizing effect. This problem is overcome by producing a diazido-terminated glycidyl azide polymer without terminal hydroxyl groups. This useful polymer is produced by reacting polyepichlorohydrin with p-toluenesulfonyl chloride in pyridine, and reacting the resulting tosylated polyepichlorohydrin with sodium azide in dimethylformamide.

Abstract: Polymers are produced from 4 and 5 member cyclic ethers, which polymers have hydroxyl functionalities of 4.

Abstract: A solvent-free molten salt method for the synthesis of glycidyl azide polymer.

Abstract: 1,5-Diazido-3-Nitrazapentane is disclosed as an energetic plasticizer, together with a method for producing same.

Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

Abstract: Novel trisubstituted phenyl analogs are now found to have activity as for the treatment of congestive heart failure.

Abstract: Energetic azido curing agents are provided for curing hydroxy-terminated aliphatic polymers having pendant alkyl azide groups.

Abstract: A method of producing a hydroxy-terminated aliphatic polyether utilizing a specific catalytic interaction to enhance the solubility and resulting reactivity of an azide moiety.

Abstract: A gas-generating agent for use in a ducted rocket engine essentially consists of an aliphatic polyester represented by the formula: ##STR1## or the formula: ##STR2## and a curing agent and optionally incorporating therein additives such as a curing catalyst.

Abstract: A method of making a product comprising poly(glycidyl azide) by reacting polyepichlorohydrin and alkali and/or alkaline earth metal azides in the presence of certain quaternary amine compounds.