112 results about "Cyclooctene" patented technology

Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and / or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.

A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.

Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

The invention belongs to the technical field of liquid crystal polymer materials, and particularly relates to a side chained linear azobenzene liquid crystal polymer material and a preparation method thereof. In the method, a novel liquid crystal polymer material using butadiene-ethylene-functional group substituted ethylene ternary alternative polymer as a main chain and the azobenzene derivative as a side chain structure is synthesized by using an open loop translocation polymerization method through using a 5-substituted cyclooctene (a substituent group is an azobenzene derivative) monomer in the presence of a Grubbs catalyst. According to the invention, the problem that the conventional azobenzene liquid crystal elastomer material is insoluble and is not molted so as not to be prepared by adopting a common machine shaping method. Under the condition of no cross-linked network structure, the side chained linear azobenzene liquid crystal polymer material has the rubber elasticity and good optical response characteristic; and the side chained linear azobenzene liquid crystal polymer material can machined to form liquid crystal polymer materials, such as films and fibers, after molten or dissolved without being limited in machining size and appearance and can be recycled for re-machine shaping after machine-shaping, and is a novel low-carbon and environment-friendly optical response liquid crystal polymer material.

Described is a pretargeting method, and related kits, for targeted medical imaging and / or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has one or more axial substituents.

The invention relates to a method for producing 1,2-dodeca-2,10-diene diacid and 1,12-dodecanoic acid whereby cyclooctene and acrylic acid are reacted with a ruthenium catalyst by way of a metathesis reaction at high substrate concentrations until the reaction takes place in substance, the resulting unsaturated dicarboxylic acid being precipitated and being hydrated in a second reaction step.

Described is a pretargeting method, and related kits, for targeted medical imaging and / or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other a cyclooctene or cyclooctyne.

Described is a pretargeting method, and related kits, for targeted medical imaging and / or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has one or more axial substituents.

Described is a method, and a combination of agents for used therein, by which an agent administered to a subject can be rapidly cleared from circulation. This is achieved by providing an Administration Agent (e.g. a probe for pretargeting) with a reactive group and providing a Clearing Agent with another reactive group, said reactive groups forming a bio-orthogonally reactive pair. Preferably, the reactive pair comprises a cyclooctene or cyclooctyn as one reactant, and a diene as the other reactant. The method and combination can be used for the removal of any bindable molecule from circulation, such as an excess of a pre-targeting probe in the course of a pre-targeting method, a targeting or imaging agent delivered, or the removal of any biomolecule already present in circulation.

The invention provides a method for preparing a sea urchin like polyaniline microspheres supported catalyst, which belongs to the technical field of polymer supported catalytic material preparation, wherein polystyrene microspheres prepared by a soap-free emulsion polymerization method are used as seeds, and sea urchin like polyaniline microspheres are prepared by a seed swelling polymerization method. The method comprises the following steps: firstly, adding aniline monomers into aqueous solution of the polystyrene microspheres, stirring the mixture for a period of time so that the aniline monomers are swelled into the polystyrene microspheres; secondly, adding the mixture into aqueous solution of iron-based oxidants so that the aniline monomers swelled into the polystyrene microspheres can react with the oxidants so as to obtain the sea urchin like polyaniline composite microspheres; and thirdly, using a catalyst MoO2(acac)2 to perform load reaction with the prepared sea urchin like polyaniline composite microspheres to syntheize a polyaniline supported molybdenum-based catalyst. When the prepared polyaniline supported molybdenum-based catalyst is used for catalyzing cyclooctene to perform epoxidation, and tert-butyl hydroperoxide is used as an oxygen source, and good catalytic activity and the recycling performance are represented.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a method for synthesizing a Ti-MWW molecular sieve hollow sphere with the high external specific surface area. The method includes the steps that reactive gel is rotated along a horizontal rotating shaft in an airtight reaction still, rotary ageing is conducted for a period of time at a certain temperature first, then rotary crystallization is carried out for a period of time at a certain temperature, and the Ti-MWW molecular sieve hollow sphere can be synthesized by reasonably adjusting the rotating speed. By the adoption of the method, a Ti-MWW molecular sieve of the hollow sphere structure can be synthesized through one step, a sacrificial template in a hard template method does not need to be used, the external specific surface area can reach up to 180-260 m<2> / g, and excellent catalytic activity can be achieved in epoxidation reactions for catalyzing chloropropene, cyclopentene, cyclohexene, cyclooctene and H2O2 (or TBHP).

Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and / or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.

Disclosed is a kit for the administration and activation of a Prodrug. The kit comprises a Masking Moiety linked, directly or indirectly, to a Trigger moiety, which in turn is linked to a Drug, and an Activator for the Trigger moiety. The Trigger moiety comprises a dienophile and the Activator comprises a diene, whereby the dienophile is an eight-membered non-aromatic cyclic alkenylene group, preferably a cyclooctene group, and more preferably a trans-cyclooctene group. The Trigger and the Activator undergo a fast, bio-orthogonal reaction resulting in the release of the Masking Moiety, and activation of the drug.

The invention provides a prodrug activation compound, which is characterized by comprising a polypeptide fragment, and a tetrazine group and a hydrophobic group which are connected to the polypeptidefragment through chemical bonds; wherein at least one phosphorylated tyrosine exists in the amino acid of the polypeptide fragment. The prodrug activation compound provided by the invention has targeting property and specificity, can be quickly and efficiently accumulated in tumor cells and is self-assembled in situ to form a nano assembly, so that a trans-cyclooctene modified anti-tumor prodrug is efficiently and specifically activated; the prodrug activating compound and the prodrug system are good in biocompatibility and free of system toxicity. A solid-phase synthesis method is adopted inthe preparation method of the prodrug activated compound, the operation is simple, and the obtained product is high in chemical purity and high in total yield.

The invention belongs to preparation of antibiotic, in particular to preparation method of Valnemulin and hydrochloride thereof.D-hydroxy valine Dane salt is added into more than ten weight of tetrahydrofuran and is suspended by stirring at 0-20 DEG C, and triethylamine, N, N-dimethyl formamide (acetamide) and N-methyl morpholine are added until reaction liquid is clear; methyl (ethyl) chloroformate molar weight of which is not more than that of D-hydroxy valine Dane salt is added; (2-amino-1, 1-dimethyl ethyl) mercaptoacetic acid, (3aS, 4R, 5S, 6S, 8R, 9R, 9aR, 10R)-octohydrogen-5, 8-dyhydroxy-4, 6, 9,10-tetramethyl-6-ethenyl-3a, 9-propane-3aH-cyclopentene (cyclooctene)-1(4H)-keto-8-ester the molar weight of which is not more than that of D-hydroxy valine Dane salt is dissolved in equal mass of tetrahydrofuran, the reaction liquid is dripped in and stirred at 0-10 DEG C, and reaction is carried out for 2-5h at 0-20 DEG C; the organic solvent is removed, the residue is added with water and hydrochloric acid is used for adjusting pH value, heating up, stirring and decontaminating are carried out, and the filtration is freeze dried to obtain Valnemulin hydrochloride. The invention solves the problems of low purity and high reaction condition of the existing product and has the advantages of simple technology and high product purity.

The invention discloses the application of biphenyl cyclooctene containing substance in the process for preparing Alzheimer disease treating medicine, wherein the substance has the formula disclosed in the specification. The biphenyl cyclooctene containing substance can effectively reduce the output of Abetta, suppress the formation of aged speckle, improve the learning and memory capability for the modeled mouse, thus achieving the goal of treating and delaying AD disease.

The invention discloses a polyacid catalyst wrapped by cadmium-based polypyridine macro ring and a preparation method thereof; according to the method, the cadmium-based polypyridine macro ring and polyoxometallate are respectively dissolved in acetonitrile solution, then mutual dripped slowly, stood, and precipitated to obtain the needed catalyst. The catalyst is used in epoxidation of cyclooctene, the conversion rate is as high as 95.11%, and the selectivity is over 95.72%. The catalyst provided by the invention not only retains excellent catalytic performances of the polyacid componnet, can realize the catalyst recovery, improves the shortcoming that traditional polyacid catalysts cannot be recycled, and has the advantages of simple preparation process and high yield.

The invention belongs to the traditional Chinese medicine pharmaceutical field and relates to a new use of a dibenzocyclooctadiene lignan in the preparation of anti-HBV drugs. The invention extracts the dibenzocyclooctadiene lignan from S.wilsoniana of Schisandra plant and confirms the anti-HBV activity thereof through a test. The result of the pharmacological test comparison of the dibenzocyclooctadiene lignan with the active controlled lamivudine proves that the dibenzocyclooctadiene lignan has significant anti-HBV role, low effective concentration and smaller cell toxicity, and the dibenzocyclooctadiene lignan can be used as an active ingredient for preparing the drugs for the treatment of hepatitis B.

A catalytic method is provided for a ring-opening cross-metathesis reaction between a cycloolefinic substrate and a second olefinic reactant, wherein the catalyst used is a transition metal alkylidene complex substituted with an N-heterocyclic carbene ligand. The substrates are selected so that the rate of the cross-metathesis reaction of the second olefinic reactant, kCM, is greater than or equal to the rate of the ring-opening metathesis reaction, kRo. In this way, the predominant ROCM product is a monomer, dimer, and / or oligomer, but not a polymer. The invention additionally provides for selective production of an end-differentiated olefinic product, using trisubstituted cycloolefins as substrates and / or a subsequent cross-metathesis reaction following an initial ROCM step. The cycloolefinic substrates include low-strain olefins such as cyclohexene as well as higher strain olefins such as cyclooctene.

The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein A is selected from the group A1 consisting of a C3-C8-cycloalkyl group or a C4-C8-cycloalkenyl group, whereby the members of C3-C8-cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C4-C8-cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving perception, concentration, learning and / or memory in patients in need thereof. Chemically, the compounds are characterised as pyrazolopyrimidinones with a cycloalkyl-moiety directly bound to the 1 position of the pyrazolopyrimidinone and a second substituent in the 6 position which is bound via an optionally substituted methylene-bridge. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.

Described is a pretargeting method, and related kits, for targeted medical imaging and / or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.

The invention relates to a method for catalyzing cyclooctene epoxidation by molybdenum polyoxometallate. The adopted technical scheme is as follows: with the molybdenum polyoxometallate based on Mo8O26 anions as catalyst, and butyl imidazole tetrafluoroborate ionic liquid as solvent, cyclooctene is added; the reaction temperature is 40-70 DEG C; the pressure is normal; the reaction time is 1.5-3 hours; epoxide can be generated with high selectivity; the ionic liquid and the catalyst can be recycled through simple treatment or no treatment; the reaction is recycled more than 5 times; the total conversion rates are all high above 95%. The technology in the catalytic process is simple; the catalyst can be recycled; at the same time of guaranteeing the catalytic effect, the cost of the catalyst is largely reduced.

The invention discloses an Au / BW11 / Al2O3 catalyst and its preparation method and use. Al2O3 is orderly loaded with BW11 and nano-gold so that the Au / BW11 / Al2O3 catalyst is formed. The Al2O3 is used as a catalyst carrier and Au and BW11 are used as catalyst main active components. The Au / BW11 / Al2O3 catalyst has high loading efficiency and a good dispersion degree. The Au / BW11 / Al2O3 catalyst has the characteristics of high activity and good selectivity of cyclooctene epoxidation preparation of epoxycyclooctane and satisfies industrial production requirements.

The invention provides compositions that may be used for imaging intracellular structures. The invention further provides methods of imaging intracellular structures. In certain embodiments, the compositions of the invention include trans-cyclooctene-containing ceramide lipids and tetrazine-containing rhodamine-related dyes.

The invention discloses a universal type multi-signal output biosensor, as well as a preparation method and application thereof. The universal type multi-signal output biosensor comprises two parts: a transcyclooctene modified vancomycin derivative used as a recognition molecule and functionalized gold and silver compound nanoparticles used as a signal conversion element, wherein the amino activated locus of the vancomycin molecule is covalently coupled with transcyclooctene; the gold and silver compound nanoparticles adopt silver shell-gold core compound nanoparticles; the surfaces of the gold and silver compound nanoparticles are simultaneously modified with a disulfide bond-containing tetrazine compound and a Raman microprobe molecule. The universal type multi-signal output biosensor can be applied to detection of Gram-positive pathogens, has the advantages of being high in efficiency, low in external environment influence, wide-spectral in targets and the like, and can meet the requirement of actual production and living.

The invention provides a 1,2,4,5-tetrazine compound for bioorthogonal reaction as well as a preparation method and application thereof, and also provides a new-structure 1,2,4,5-tetrazine compound labeled by <99m>Tc / Re, a preparation method thereof and application thereof in bioorthogonal reaction-based developing, and particularly in brain developing. The structure of the labeled compound is as shown in a formula (I) which is shown in the description. A reaction kinetics experiment shows that molecules and trans-cyclooctene derivatives have very high reaction activity, an in-vivo biodistribution experiment of normal mice shows that the molecules labeled by the <99m>Tc can effectively pass through blood brain barrier, and brain elimination is also faster, so that the 1,2,4,5-tetrazine compound can be a novel developing agent for intracerebral bioorthogonal reaction.

An application of 1-hydroxy-2,3,12,13,14-pentamethoxy-6- hexanoately-7-hydroxy-8-methyl-9-benzoately-biphenyl cyclooctadiene lignan, white is extracted from schisandra propinqua, in preparing antineoplastic medicines is disclosed.

A process to produce an ionomer comprising reacting alkyl-cis-cyclooctene and cis-cyclooctene in a mole ratio from 1:0 to 0:1, in the presence of a difunctional chain transfer agent under ring opening metathesis polymerization conditions to form an unsaturated polyolefin reactive telechelic pre-polymer; hydrogenating the unsaturated polyolefin reactive telechelic pre-polymer to produce a hydrogenated polyolefin reactive telechelic pre-polymer; reacting the hydrogenated polyolefin reactive telechelic pre-polymer with at least one compound according to the formula aMx·b(R)y, wherein M is a metal, x is a charge of M, R is an alkyl, aryl, oxide, or fatty acid, y is a charge of R, a and b are integers of at least 1, and ax+by=0, to form an ionomer is provided. Further provided are ionomers produced thereby.