42results about How to "High labeling yield" patented technology

The invention discloses a targeted probe for nuclide labeling and a preparation method and an application of the targeted probe. A general structural formula of a complex is as shown in the specification, wherein R' is a nuclide chelating group; R is a targeted group; Dn is a molecular skeleton which is formed by repeated michael addition reaction and amidation reaction employing propargylamine as an initial reactant, the peripheral group is amino, n represents different algebras, and the numerical value of n is an integer greater than or equal to 0; and m is equal to 2n. A polymer in the targeted probe for nuclide labeling is beneficial to improvement of the specific activity; a high-quality developing result can be obtained by instrument scanning; the targeted probe can play a role in effectively monitoring tumors or inflammatory diseases; meanwhile, carrying of relatively many nuclides on a molecule is facilitated by the formed polymer; the nuclide concentration of focus location is improved; and the targeted probe plays a relatively good treatment role.

{0><}0{>The invention discloses a radio-labeled tumor developing agent as well as a preparation method and application thereof. <0}{0><}0{>The radio-labeled tumor developing agent structurally contains an alpha-amino acid derivate structure capable of labeling nuclide and a tumor-targeted folic acid molecule, wherein radionuclide is 18F, and the alpha-amino acid derivate structure and the folic acid molecule are connected in a specific chemical mode. <0}{0><}0{>The invention further relates to a preparation method of the compound and application of the compound serving as a tracing developing agent in PET development in a human body or an animal body. The radio-labeled tumor developing agent has the advantages of simplicity in preparation, low price and strong targeting property especially when serving as a tumor developing agent.

The invention provides a novel carbazole fluorescent thiol marking reagent as well as a synthesis method and application thereof. The florescent marking reagent adopts carbazole as a fluorescent basering and activated C=C double bonds as reaction activity groups, is simple and convenient in synthesis step, easy to operate and can be synthesized in a large scale through two steps of reactions as follows: (1) enabling carbazole to react with 4-bromobenzaldehyde so as to obtain an intermediate (4-(9H-carbazole-9-yl) benzaldehyde; (2) enabling the intermediate (4-(9H-carbazole-9-yl) benzaldehydeto react with malononitrile so as to obtain a target product (4-(9H-carbazole-9-yl) benzaldehyde malononitrile, and performing recrystallization for three times with acetonitrile, thereby obtaining ayellow needle-shaped crystal. The chemical purity of the fluorescent marking reagent provided by the invention is up to 99%, and the fluorescent marking reagent is stable in chemical property. The novel carbazole fluorescent thiol marking reagent provided by the invention is capable of rapidly and accurately marking degradation thiol products of organic thiol ester insecticides under a gentle condition, and quantitative analysis on contents of organic thiol ester insecticides in reagent samples can be achieved.

The present invention relates to Halogenated amino acid analogues for use in diagnosis, which compounds have the general formula (I) wherein: R is (C1–C6) alkyl optionally substituted with thioether or ether oxygen atom when n=0, or a substituted aromatic or heteraromatic ring when n=1–6; and m=0 or 1; and X is a halogen atom. The invention further relates to precursor compounds for these analogues, to a method of preparing these analogues, to a pharmaceutical composition comprising these analogues and to the use of these analogues and compositions in the diagnosis of cancer

The invention discloses a radioactive label tEB-TMTP1 compound. Through modification with DOTA and NOTA bifunctional chelating agents, DOTA-tEB-TMTP1 and NOTA-tEB-TMTP1 are synthetized, radioactive metal nuclides of radioactive nuclides 68Ga, 64Cu and 177Lu and the like are respectively labelled, and a nuclear medicine diagnosis and treatment probe of specific target high-metastasis tumors is synthetized. The probe designed and synthesized from the radioactive label tEB-TMTP1 compound disclosed by the invention has two advantages that firstly the labelling steps are simple, higher labelling production rate is achieved, and a foundation is laid for clinical application; secondly, the obtained DOTA-tEB-TMTP1 probe and the obtained NOTA-tEB-TMTP1 probe have excellent pharmacokinetics nature,the half life of the DOTA-tEB-TMTP1 probe and the obtained NOTA-tEB-TMTP1 probe in bodies can be notably prolonged, the DOTA-tEB-TMTP1 probe and the obtained NOTA-tEB-TMTP1 probe can circulate in thebodies for a long term, tumor part ingestion is increased, and target treatment on high-metastasis tumors can be realized.

The invention discloses a two-dimensional palladium-based probe with radioiodine labeling and a preparation method and application of the probe. The probe comprises a two-dimensional palladium-based nanomaterial, a PEG linking molecule, a targeting group R and radioiodine, a thiol group is arranged at one end of the PEG linking molecule, a modifiable group is arranged at the other end of the PEG linking molecule, one end of the PEG linking molecule is linked to the two-dimensional palladium-based nanomaterial through the above thiol group, the other end is linked to the targeting group R through the modifiable group, and radioiodine is directly labelled on the two-dimensional palladium-based nanomaterial. According to the present invention, a plurality of radioiodine can be carried on a unit of nanocarrier based on the strong binding force between the two-dimensional palladium-based nanomaterial and halogen ions, the probe has the characteristics of strong labeling ability, short labeling time, high labeling yield and no need of subsequent purification before application, and is more conducive to commercial application and clinical promotion of markers.

The invention discloses a one-step fluorescence derivation method of reducing sugar and application thereof. By adopting reducing sugar as a raw material, the reducing sugar and a fluorescence labeling reagent fluorescein-5-amino-thiourea are subjected to a stirring reaction at room temperature to generate a sugar-FTSC derivative so that and various types of sugar such as lactose, uronic acid, maltodextrin and traditional Chinese medicine source reducing polysaccharide are labelled. Mass spectrum structure analysis, fluorescence spectrum and microscopic living cell imaging research are performed on an obtained product. Results show that the carbohydrazone derivative obtained by labeling has good stability and high fluorescence yield, and can be used for fluorescence derivative labeling andmicroscopic fluorescence imaging detection of reducible neutral and acidic oligosaccharides. The method has the advantages of mild reaction conditions, high reaction yield and simple operation, and can be used for large-scale synthesis and preparation of functional oligosaccharide probes; meanwhile, the method is suitable for researching mass spectrometry, chromatography, fluorescence, microscopic fluorescence imaging, flow cytometry and the like of reductive oligosaccharides and polysaccharide molecules, and has a wide application prospect in the field of life science.

A novel gall bladder image agent which includes a radio-labelled MAG3-tri-galactosamine, and its preparation method, which includes reacting mercaptoacetyltriglycine (MAG3)-tri-galactosamine, SnF2 and Tc-99m in the presence of a phosphate buffer solution (at pH of from 10.0˜12.0) to obtain Tc-99m-MAG3-tri-galactosamine, when the MAG3-tri-galactosamine is MAG3-DCM-Lys(Gah-GalNAc)3 (where DCM represents a dicarboxymethyl group, and Gah represents a glycine-aminohexyl group), it obtains a labelling yield of at least 90%, and its specific radioactivity is at least 7.0×109 Bq / mg.

The invention provides an RGD polypeptide coordination complex of a radioactive nuclide label. According to the structure of the coordination complex, the radioactive nuclide is selected from 64Cu, 68Ga, 111In, 62Cu, 67Cu, 67Ga, 86Y, 89Zr or 18F; the ligand is a ligand compound containing an RGD structure, which is shown in a formula (I). The coordination complex has stronger ligand stability and high target / non-target ratio, and the appetency of the ligand with integrin AlphavBeta3 is stronger. The invention further provides a preparation method of the coordination complex, and an application of the coordination complex in preparing tumor developers.

A novel gall bladder image agent which includes a radio-labelled MAG3-tri-galactosamine, and its preparation method, which includes reacting mercaptoacetyltriglycine (MAG3)-tri-galactosamine, SnF2 and Tc-99m in the presence of a phosphate buffer solution (at pH of from 10.0˜12.0) to obtain Tc-99m-MAG3-tri-galactosamine, when the MAG3-tri-galactosamine is MAG3-DCM-Lys(Gah-GalNAc)3 (where DCM represents a dicarboxymethyl group, and Gah represents a glycine-aminohexyl group), it obtains a labelling yield of at least 90%, and its specific radioactivity is at least 7.0×109 Bq / mg.

The present invention relates to a method for preparing a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical using selective azide substitution reaction, the method comprising: a first step for obtaining [<18>F]fluoride from a cyclotron through a <18>O(p, n)<18>F reaction; a second step for obtaining a [<18>F]F- / H2 18O solution by separating the [<18>F]fluoride using an acetonitrile reaction solution in which K2.2.2 and K2CO3 are dissolved; a third step for obtaining K2.2.2 / K<18>F by heating the [<18>F]F- / H2<18>O solution; a fourth step for obtaining a first precursor solution by adding the K2.2.2 / K<18>F and a bis(toxyloxy)methane compound into a reactor and adding a reaction solvent thereto to cause reaction; a fifth step for obtaining a [<18>F]fluoromethyltosylate compound by cooling the first precursor solution and adding an azide reagent thereto to cause azide substitution reaction.

The present invention relates to carbazole fluorescent thymine drug labeling reagent, synthesis and application. Carbazole is used as fluorescent mother ring, benzyl chloride is used as reactive group, and its chemical name is: 4-(9H-carbazole-9- base) benzyl chloride. The novel stable carbazole-based fluorescent thymine drug labeling reagent described in the present invention can accurately, sensitively and rapidly label thymine drugs under mild conditions, thereby realizing the separation of micro and trace amounts of thymine drugs in complex systems It can be used in research fields such as environmental analysis and food safety, and has broad application prospects.

The invention discloses a nuclide-labeled targeted probe compound as well as a preparation method and application thereof. The molecular weight of the nuclide-labeled targeted probe compound is 1kDa-50kDa, and the nuclide-labeled targeted probe compound comprises a polyethyleneimine skeleton and a targeted group derived from N-acetyl glucosamine or diacetyl chitobiose acid and is labeled through coordination of a radionuclide X label and an imino group on the polyethyleneimine skeleton. The nuclide-labeled targeted probe compound can be applied to in-vivo hepatic fibrosis detection, has the advantages of relatively short imaging time, relatively high imaging quality, relatively wide imaging depth, less kidney radioactive accumulation and the like, and is relatively beneficial to early hepatic fibrosis. Meanwhile, by combining with CT imaging, accurate anatomical structure signals and functional information can be obtained, thereby being beneficial to the evaluation and accurate staging of hepatic fibrosis.

The invention relates to the technical field of organic small molecule isotope labeling, in particular to a stable isotope mercapto compound labeling reagent, a synthesis method and application thereof. The isotope labeling reagent is [d0] / [D4]-acridone-10-ethyl-N-maleimide. The reagent adopts acridone as the isotope group and takes maleimide as the reaction group. The synthesis method includes: taking [d0] / [D5]-bromobenzene as the raw material, and carrying out two-step condensation reaction, hydroxylation reaction, helogenation reaction, Gabriel reaction and acylation reaction, thus obtaining the reagent. The stable isotope deuterium label obtained by the invention is subjected to separation and purification, then the isotope labeling position is table, the chemical purity is up to 99.0% or more, and the isotope abundance is up to 99.0% or more. The reagent can selectively label mercapto compounds, and has the advantages of fast labeling reaction rate, high labeling yield and high mercapto selectivity, etc.

The invention discloses a [18F]AlF-labeled PET polypeptide probe and a preparation method thereof, comprising TMTP1 polypeptide and NOTA linked together, and its structural formula is as follows:. In the present invention, G-TMTP1 polypeptide is designed by adding a glycine to TMTP1 so that it does not affect its biological activity after being radiolabeled, and uses 18F as the radionuclide, and uses [18F]AlF-NOTA to mark G-TMTP1 Polypeptide, the obtained [18F]AlF-labeled PET polypeptide probe has excellent pharmacokinetic properties, fast background clearance rate, low liver uptake, good stability in vivo, high uptake in tumor sites, and high specificity for diagnosis Metastatic tumors can be used for the diagnosis or curative effect evaluation of highly metastatic malignant tumors.