11 results about "Bifunctional reagent" patented technology

The invention concerns homogenous antibody-conjugates with high payload loading (high DAR) obtained by site-specific conjugation to a single antibody N-glycan. The conjugates according to the invention are homogeneous, i.e. have a DAR at or close to the theoretical DAR with a narrow distribution, and do not require any genetic modification of the antibody. The invention further concerns a modular, non-genetic preparation method for such conjugates, involving three simple steps and starting from any antibody. These steps are (a) enzymatic remodeling of the glycan to give an antibody functionalized with two or four click probes per antibody, (b) strain-promoted cycloaddition with a multivalent, bifunctional reagent comprising one cyclic alkyne and at least two click probes that are not reactive towards the cyclic alkyne, and (c) inverse electron-demand Diels-Alder cycloaddition of the click probes with branched linker-drug constructs comprising one cyclic alkyne or strained alkene, connected to one or more payloads preferably connected through a cleavable linker. The resulting conjugates, with DAR6 or higher, are rapidly generated with high homogeneity and with surprising stability. In addition, HIC profiles of the resulting ADCs indicate small relative retention time and therefore show high potential in the targeting of tumour cells and / or the treatment of cancer.

The invention provides an aryl alkyl ketoxime derivative as well as a preparation method and application thereof, and relates to the field of aryl oxime derivatives. The preparation method of the aryl alkyl ketoxime derivative comprises the following steps: by taking potassium formate as an additive, carrying out free radical reaction on a compound I and a compound II under ultraviolet irradiation in the presence of tert-butyl nitrite to obtain the aryl alkyl ketoxime derivative, the compound I is substituted iodobenzene or iodopyridine; the compound II is substituted styrene or thienyl ethylene; wherein a hydrogen atom transfer / single electron transfer relay sequence is utilized to activate a compound I, and tert-butyl nitrite is adopted as a bifunctional reagent, and is used as a hydrogen atom transfer reagent and an oxime source. According to the preparation method of the aryl alkyl ketoxime derivative, pre-functionalization is not needed, a reaction substrate is wide in universality and good in compatibility, reaction conditions are mild, operation is easy and convenient, a target product can be efficiently and rapidly prepared on the premise of high yield, and a new way is provided for oxime synthesis.

The present invention relates to homogeneous antibody-conjugates with high payload loading (high DAR) obtained by site-specific conjugation with a single antibody N-glycan. The conjugates according to the invention are homogeneous, i.e., with a DAR equal to or close to the theoretical DAR and narrow distribution, and do not require any genetic modification to the antibody. The invention also relates to a modular, non-genetic preparation method for such a conjugate, which method comprises three simple steps and can start from any antibody. These steps are (a) enzymatic remodeling of the glycan to give antibodies functionalised per antibody with two or four click probes, (b) strain-promoted cycloaddition with a multivalent bifunctional reagent comprising a cyclic alkyne and at least two click probes that are not reactive to the cyclic alkyne, and (c) strain-promoted cycloaddition with a multivalent bifunctional reagent comprising at least one cyclic alkyne and at least two click probes that are not reactive to the cyclic alkyne. And (c) subjecting the click probes to reverse electron demanding Diels-Alder cycloaddition with branched linker-drug constructs comprising a cyclic alkyne or strained olefin, linked to one or more payloads, preferably by cleavable linkers. The resulting conjugates have a DAR of 6 or higher, are rapidly generated, have high homogeneity and surprising stability. In addition, the HIC profile of the resulting ADC shows a relatively short retention time, and thus shows a very high potential in targeting tumor cells and / or treating cancer.

The invention discloses preparation and stabilization methods of an INO3 solution and application of the INO3 solution. The preparation method comprises the following steps: dissolving silver nitrate in a first organic solvent to form a silver nitrate solution; dissolving an iodine elementary substance in a second organic solvent to form an iodine elementary substance solution; mixing the silver nitrate solution with an iodine simple substance solution, and carrying out a reaction according to a reaction equation AgNO3 + I2-AgI + INO3; and separating AgI precipitate generated by the reaction to obtain an INO3 solution. When a non-acetonitrile solvent is used, acetonitrile needs to be added as a stabilizer, so that the volume content of acetonitrile in the final solution is greater than or equal to 50%. The INO3 solution can be used as a bifunctional reagent for synchronous iodination and nitration reactions of aromatic compounds. The half-life period of the INO3 solution prepared by the method provided by the invention in an acetonitrile system under the dark condition of 25 DEG C reaches 48.5 days, the product stability is good, the INO3 solution has excellent activity on the bifunctionalization reaction of aromatic compounds such as phenol, and nitrophenol and iodo-phenol products can be generated at the same time.

The invention belongs to the technical field of environmental analytical chemistry and detection, discloses a soil and water polychlorinated naphthalene environment rapid detection method, and aims to solve the problems that an existing polychlorinated naphthalene detection method is complex in sample pretreatment, long in detection period and high in cost, and a rapid detection technology is insufficient in sensitivity, weak in anti-interference capability and the like. The method comprises the following steps: constructing a free radical chain reaction kinetics system consisting of a chain initiator, a signal report molecule, a chain transfer and regeneration bifunctional reagent and a pH buffer system, taking polychlorinated naphthalene as a chain terminator, and determining the fluorescence quenching rate change of the signal report molecule after the polychlorinated naphthalene is introduced by measuring the fluorescence quenching rate change of the signal report molecule. The ultrasensitive quantitative detection of polychlorinated naphthalene in soil and water is realized. By adopting the technical scheme, the method has the advantages of high sensitivity and signal amplification effect, no need of complex sample pretreatment, environment friendliness, quick response, excellent anti-interference performance and the like.

The application discloses a kind of reduced graphene oxide aerogel and its preparation method and application, including the compound with mercapto and water are mixed, and mercapto functionalized carbon quantum dot solution is prepared by hydrothermal reaction;And graphene oxide is dispersed in water, and obtain graphene oxide dispersion;The obtained mercapto functionalized carbon quantum dot solution is mixed with graphene oxide dispersion, and hydrothermal reaction is carried out after adjusting pH to alkaline, and form hydrogel precursor;The precursor is solvent exchanged and freeze-dried, and reduced graphene oxide aerogel is obtained.The application first uses mercapto functionalized carbon quantum dots (SH-CDs) as "reduction-crosslinking" bifunctional reagent, constructs rGO aerogel with high conductivity, complete three-dimensional interconnected network structure, the whole preparation process does not need to add additional toxic reducing agent or crosslinking agent, process is simple, environmental protection.Prepared reduced graphene oxide aerogel has good terahertz absorption and shielding performance.

The invention discloses a preparation method of an On-DNA halogen-halogen coupling compound, which comprises the following steps: taking an On-DNA aryl halide as a substrate, reacting with an acid aryl halide compound under the conditions of alkali, a boron-containing compound and a palladium catalyst, realizing in-situ conversion of halogen into a boric acid (ester) bifunctional reagent through a one-pot method, and further obtaining the On-DNA halogen-halogen coupling compound through Suzuki reaction. The reaction method is high in yield, wide in substrate universality, mild in condition, convenient to operate and suitable for synthesis of the DNA coding compound library through a porous plate.

The invention discloses a covalent modification method of a high-performance lignin-based electrode material, and belongs to the technical field of biomass-based supercapacitors. The method specifically comprises the following steps: dissolving sulfate lignin in DMF (Dimethyl Formamide), adding a bifunctional reagent, and stirring for reaction; and after the reaction is finished, pouring the reaction liquid into deionized water in which hydrochloric acid is dropwise added, and carrying out anti-precipitation, filtration, drying, heat treatment, activation and other processes to obtain the covalent modified lignin. The modified lignin, a conductive agent and a binder are ground and mixed, a current collector is coated with the mixture and dried, and the lignin-based electrode is obtained. The covalent modification degree of the lignin is regulated and controlled by controlling the adding amount of the bifunctional reagent, modified lignin with different thermodynamic properties is obtained, and the purpose of regulating and controlling lignin derived carbon structure defects is achieved. The preparation method is controllable in scale and simple to operate, the obtained electrode material is few in defect structure and excellent in electrochemical performance, and a new theory and a new method are provided for development of the lignin-based electrode material.

The invention relates to the technical field of bioactive component extraction, in particular to a method for extracting auricularia auricula polysaccharide from auricularia auricula, which comprises the following steps: firstly, adding a specific synergist A into cleaned and crushed auricularia auricula, and carrying out ultrasonic-assisted pretreatment; adding a special compound enzyme and a regulating agent B, and carrying out microwave radiation enzymolysis; extracting by using hot water and adding a bifunctional reagent C, concentrating by using a nanofiltration membrane, and finally performing alcohol precipitation, washing and vacuum drying to obtain a product. The extraction method has a remarkable effect; the extraction efficiency can be greatly improved, and the polysaccharide purity and activity are improved; cost, raw material and energy consumption and enzyme consumption can be reduced, acid-base pollution is avoided, and the method is suitable for industrial production.

The application discloses a 3-bromo-5-methylene pyrrolone hetero-difunctional reagent, a preparation method thereof and application thereof in biological coupling. The reagent comprises a specific structure as shown in a general formula (I) and covers various variant forms. The preparation method comprises a plurality of reaction steps, and the reagent is prepared from a compound containing a specific functional group through a series of reactions. The reagent performs well in biological coupling and can be used in biological coupling of oligonucleotides and cell-penetrating peptides and proteins and polypeptide cyclization. In the biological coupling of oligonucleotides and cell-penetrating peptides and proteins, efficient modification and coupling can be realized, and the conjugate can maintain good biological functions. In polypeptide cyclization, linear peptides can be efficiently cyclized and cell targeting can be maintained. The application provides a new way for biological coupling technology and has important application prospects in the fields of biomedical research and drug research.

The invention discloses a magnetosome-based GPC3 thermal dissociation aptamer composite magnetic bead, and relates to the technical field of biological medicines. The magnetosome-based GPC3 thermal dissociation aptamer composite magnetic bead comprises a temperature-sensitive thermal dissociation aptamer for specifically recognizing GPC3 protein, a magnetosome and a bifunctional reagent. The invention further provides a preparation method and application of the GPC3 thermal dissociation aptamer composite magnetic bead based on the magnetosome. The magnetosome-based GPC3 thermal dissociation aptamer composite magnetic bead prepared by the method provided by the invention can be specifically bound with GPC3 at 37 DEG C and dissociated with GPC3 at 46 DEG C, so that effective release of drugs in magnetocaloric therapy is realized, and the problem that a thermal dissociation aptamer capable of being specifically bound with GPC3 protein is lacked in the prior art is effectively solved.