65results about How to "High radiochemical purity" patented technology

The invention discloses a preparation method and application of a pyridazinone myocardial perfusion PET radiopharmaceutical. According to the invention, a large-dose initial 18F activity label is adopted, the precursor usage amount of a reaction, the reaction temperature and the purification HPLC condition are optimized, the reaction yield is improved, the preparation amount of [18F]Fmpp2 can reach 200 mCi, the chemical impurity amount is reduced, the radiochemical purity is high, and the key quality index is kept stable within 6 hours. A method for preparing a [18F]Fmpp2 solution for injection is improved, and the radiochemical purity and stability of the [18F]Fmpp2 are improved. The [18F]Fmpp2 prepared by the invention is subjected to miniature pig myocardial model PET imaging display; after the [18F]Fmpp2 is intravenously injected, the myocardial radioactive uptake is high, and the influence of peripheral organs on myocardial development is small; and normal myocardium, ischemic myocardium caused by chronic coronary artery stenosis and infarcted myocardium caused by acute coronary artery stenosis can be distinguished.

The invention relates to a radioactive fluorine labeled Larotrectinib compound and a preparation method thereof, in particular, an in vivo imaging agent for Trk receptor subtype in refractory solid tumors, the present invention provides a radiofluorocompound 18F-Larotrectinib and 18F-Larotorectinib analogues based on a novel inhibitor Larotrectinib for tyrosine receptor kinase (TRK), and more particularly a preparation method of the Larotrectinib and its analogue radioactive fluorine-18 labeled compound 18F-Larotdirectinib and its 18F-Larotorectinib analogue. Compared with the prior art, the invention has the advantages of fast reaction speed, relatively mild condition, simple operation, short reaction time and simple post-treatment, and the prepared carrier-free radioactive label compounds have high radiochemical purity and positron emission characteristics, and PET-CT positron emission tomography can be used, so as to visually display the distribution of Larotrectinib compounds and their analogues in vivo and tumors, and a new imaging agent for early diagnosis of tumors is provided.

The invention discloses novel radioactive 18F labeled amino acid derivatives, which are used in research on tumor positron emission tomography (PET) imaging. The derivatives are characterized in that one end of the derivatives is provided with F substituted alkoxy benzoyl structure, and the other end of the derivatives is provided with alpha-amino acid structure; substituent R1 is positioned on an alpha site of carboxyl group and is hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methylthio-ethyl group, methyl acetate group or propionate carbomethoxy group; R2 is methoxy group; and n is a number between 1 and 5. The R1 is hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methylthio-ethyl group, methyl acetate group or propionate carbomethoxy group; the R2 is hydrogen; and the n is a number between 1 and 5. Compounds improve fat solubility. Different amino acid structures are introduced into the structure, and F in the structure is 19F and 18F. Compared with the prior art, the 18F labeled amino acid derivatives provided by the invention have better discrimination degree of biological distribution, the potential of being used as a tumor imaging agent (particularly a brain tumor imaging agent), as well as the characteristics of simple preparation and high labeling rate. The R1 is hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methylthio-ethyl group, methyl acetate group or propionate carbomethoxy group; the R2 is methoxy group; and the n is a number between 1 and 5. The R1 is hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, methylthio-ethyl group, methyl acetate group or propionate carbomethoxy group; the R2 is hydrogen; and the n is a number between 1 and 5.

The invention discloses novel radioactive 18F labeled aromatic amino acids, which is characterized in that one end of the acids is provided with F substituted alkoxy benzoyl structure, and the other end of the derivatives is provided with alpha-amino acid structure; substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; R2 is methoxyl group; and n is a number between 1 and 5. The substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; the R2 is methoxyl group; and the n is a number between 1 and 5. Compounds improve fat solubility. Different amino acid structures are introduced into the structure, and F in the structure is 19F and 18F. The substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; the R2 is methoxyl group; and the n is a number between 1 and 5. The substituent R1 is positioned on an alpha site of carboxyl group and is phenyl group, benzyl group or 3-indole methyl group; the R2 is methoxyl group; and the n is a number between 1 and 5. Compared with the prior art, the 18F labeled amino acid derivatives provided by the invention have better discrimination degree of biological distribution, the potential of being used as a tumor imaging agent (particularly a brain tumor imaging agent), as well as the characteristics of simple preparation and high labeling rate.

The invention discloses a preparation method and application of a 99mTc-marked hydrazino nicotinamide-folate coordination compound. In the preparation method, the target coordination compound is obtained through two steps of synthesizing ligand hydrazino nicotinamide-folate and marking the hydrazino nicotinamide-folate by 99mTc. The coordination compound has the advantages of high hydrazino nicotinamide-folate, good stability, low cost, high tumor uptaking, good detention and good target/non-target ratio of tumor/blood, tumor/muscle and the like and can be used for preparing a tumor developer as a novel 99mTc-marked folate receptor.

A Cu(I)-Catalyzed Azide-Alkyne Cycloadditions (CuAAC) ligand comprising: a catalytic core; a fluorous tag; and a linker binding the fluorous tag to the catalytic core. A method for carrying out a Cu(I)-Catalyzed Azide-Alkyne Cycloaddition reaction, comprising: combining in a solution an alkyne-tagged component, an azide-tagged component and a Cu(I)-Catalyzed Azide-Alkyne Cycloadditions (CuAAC) ligand comprising: a catalytic core; a fluorous tag; and a linker binding the fluorous tag to the catalytic core; filtering the solution through a solid phase extraction filter to remove Cu(I)-ligand catalyst and/or excess ligand.

The invention belongs to the field of radiochemical synthesis, and particularly relates to a method for preparing tritium-labeling aditoprim. The aditoprim is used as a raw material, after the aditoprim is subjected to amino protection, a bromination reaction is conducted on the aditoprim, 2-bromine-aditoprim is obtained, then Pd/C is used as a catalyst, tritium-halogen exchange is conducted between the 2-bromine-aditoprim and halogen, and the tritium-labeling aditoprim with a high radiochemical purity being larger than or equal to 99.2%, a high chemical purity being larger than or equal to 99% and a high specific activity being 34.4 Ci/g is obtained. According to the method, a material base is provided for search and discovery of a pharmacology and toxicology effect target in the body of a new drug aditoprim and disposal of absorption, distribution, metabolis, excretion and the like of the new drug aditoprim in animal bodies, and reference is also provided for isotope labeling of drugs of the similar structures is also provided.

The invention discloses a fluorine-18-labeled spiropiperidine sigma-1 receptor compound and its preparation method and use. The preparation method comprises synthesis of a receptor ligand Spiro-OCH3(R=OCH3), synthesis of a receptor ligand Spiro-PEG1-F, synthesis of a compound intermediate Spiro-OH, synthesis of a receptor ligand Spiro-PEG2-F, synthesis of a receptor ligand Spiro-PEG3-F, synthesis of a labelled precursor Spiro-PEGn(n=1)-OTs, synthesis of a labeled precursor Spiro-PEGn(n=3)-OTs and preparation of the fluorine-18-labelled spiropiperidine sigma-1 receptor compound. The fluorine-18-labelled spiropiperidine sigma-1 receptor compound has high affinity and selectivity to a sigma-1 receptor. Through fluorine-18 labeling, the fluorine-18-labelled spiropiperidine sigma-1 receptor compound has a high labeling rate, high radiochemical purity and excellent biological properties and can be widely used for preparation of a positron imaging agent.

The present invention provides a method for the generation of ²²³Ra of pharmaceutically tolerable purity comprising i) preparing a generator mixture comprising ²²⁷Ac, ²²⁷Th and ²²³Ra; ii) loading said generator mixture onto a strong base anion exchange resin; iii) eluting said ²²³Ra from said strong base anion exchange resin using a first mineral acid in an alcoholic aqueous solution to give a first eluted ²²³Ra solution; iv) loading the ²²³Ra of the first eluted ²²³Ra solution onto a strong acid cation exchange resin; and v) eluting the ²²³Ra from said strong acid cation exchange resin using a second mineral acid in aqueous solution to provide a second eluted solution. The invention additionally provides products of corresponding purity and/or products obtained or obtainable by such a method.

The invention relates to a tumor positron emission tomography(PET) imaging agent <68>Ga-NOTA-ADG and a preparation method and application thereof, and relates to synthesis of a labeling precursor of the PET imaging agent <68>Ga-NOTA-ADG and radiosynthesis of the <68>Ga-NOTA-ADG, wherein the precursor is used for labeling the <68>Ga-NOTA-ADG for the first time, and a result shows that the radiochemical yield of the preparation method is close to 100%. The positron imaging agent <68>Ga-NOTA-ADG provided by the invention can be used as a PET imaging probe for targeting tumors. Therefore, the <68>Ga-NOTA-ADG becomes a PET candidate imaging probe for the tumors. According to the invention, the radioactive chemical synthesis of the <68>Ga-NOTA-ADG is carried out for the first time, the preparation method is simple and rapid, and a foundation is laid for scientific research and clinical application of the <68>Ga-NOTA-ADG.

An object of the present invention is to provide a method of producing liposome wherein a complex of a short half-life metallic radioactive nuclide such as ^99mTc and CD is encapsulated, with radiochemical yield and purity enabling practical application. The present invention provides a method of producing a liposome wherein a complex of a short half-life metallic radioactive nuclide and ethylenedicysteine (CD) is encapsulated, which comprises mixing a complex of a short half-life metallic radioactive nuclide and N-[2-(1H-pyrrolylmethyl)]-N′-(4-penten-3-on-2)-ethane-1,2-diamine with an ethylenedicysteine (CD)-encapsulated liposome, and incubating the mixture.

The invention belongs to the field of radiochemical synthesis, and particularly relates to a synthesis method of radioactive isotope carbon-14 labeled Dufulin (N-[2-(4-methyl[phenyl-U-<14>C<6>]benzothiazolyl)]-2-amino-2-fluorophenyl-O,O-diethylmethylphosphonate). According to the method, a feasible and economic method is provided for synthesizing the carbon-14 label of a benzene ring in a benzothiazole fragment in a chlorpyrifos molecule for the first time. The method is characterized in that radioactive isotope carbon-14 labeled benzene is used as a radioactive isotope raw material, and the target product carbon-14 labeled Dufulin is obtained by carrying out reactions such as benzene carboxylation, methylation, amination, cyclization, nucleophilic substitution and the like. The carbon-14labeled Dufulin disclosed by the invention can be used as a radioactive tracer, and is mainly used in research of metabolism and residue of Dufulin in organisms (plants, mammals and poultry) and in research of environmental behaviors of the Dufulin in soil and water bodies; and meanwhile, the invention establishes a preparation method of some carbon-14 containing synthetic building blocks.

The invention discloses a <99m>TcN-CPF2XT complex, as well as a preparation method and application thereof. Ciprofloxacin containing a quinolone pharmacophoric group is converted into a ciprofloxacinxanthate ligand (CPF2XT) capable of being complexed with <99m>Tc, and a <99 m>TcN-CPF2XT complex is obtained by using a preparation process that an S atom in the CPF2XT ligand is complexed with [<99m>TcN]<2+> nuclear. The complex is a hydrotropic substance, and is high in radiochemical purity, good in stability, and simple and convenient to prepare; the complex is highly taken and retained at thebacterial inflammation part; the ratios of inflammation/muscle and inflammation/blood are high; bacterial inflammation can be distinguished from non-bacterial inflammation; and the complex can be used as a novel bacterial inflammation photographic developer to be popularized and applied.

The invention discloses a compound SPIO-NOTA-68Ga and a preparation method thereof. The preparation method comprises the steps of using a polyethylene glycol derivative (PEG2000) modified SPIO surface amidogen for coupling a bifunctional chelating agent 1,4,7-triazacyclononane-1,4,7-nitrilotriacetic (NOTA) into the nanometer surface so as to obtain a labelled precursor SPIO-PEG2000-NOTA; then adopting 68Ga for radiolabeling SPIO to obtain the SPIO-NOTA-68Ga. In addition, the invention discloses application of the SPIO-NOTA-68Ga. Through researching in-vitro and partial in-vivo biological properties, a result shows that the SPIO-NOTA-68Ga has favorable physicochemical property and biocompatibility, higher in-vitro stability, favorable water solubility, and high labeling rate, has no need to be purified, and can be applied in research of subsequent PET/MRI bimodal development when being used as a PET/MRI bimodal probe.

The invention provides a 18F marked methylguanidine substituted benzene analogue, the structure is shown as in the general formula I, wherein a fluoro-polyethylene glycol chain is located on the para-position, bonded with guanidine methyl, of a benzene ring, n is 2-5, and F is 18F. The 18F marked methylguanidine substituted benzene analogue has the advantages of high radiochemical purity, good stability, high initial uptake value of heart, high ratio of target to non-target, long detention time and the like, and can be applied as a novel fluorine marked PET cardiac nerve receptor photographicdeveloper to the fields of radiopharmaceutical chemistry and clinic nuclear medicines.

The invention discloses a < 99m > Tc-labeled isonitrile-containing ferricyanide derivative and a preparation method and application thereof, ferricyanide with bacterial specificity (Ferrioxamine B) is converted into isonitrile ferricyanide (CNFO) capable of being complexed with < 99m > Tc, and a < 99m > Tc-CNFO complex is obtained through a preparation process that isonitrile groups in a CNFO ligand are coordinated with < 99m > Tc. The complex is a hydrophilic substance, is high in radiochemical purity, good in stability, simple and convenient to prepare, high in uptake and good in retention at bacterial inflammation parts, good in inflammation/muscle ratio, capable of distinguishing bacterial inflammation and non-bacterial inflammation, and capable of serving as a novel bacterial inflammation imaging agent to be popularized and applied.

The invention discloses a TcO nucleus marked ciprofloxacin dithiocarbamate complex and a preparation method and applications thereof. The complex uses the TcO nucleus as a central nucleus; and four sulphur atoms in two CPFXDTC ligand molecules generate complexation reaction with Tc to obtain a TcO-CPFXDTC complex. The complex has the advantages of high radiochemical purity, good stability, high intussusception of inflammation, rational target-to-nontarget ratio of inflammation to muscle, and low intussusception of liver, lung, spleen and the like. Therefore, the complex is a new developer of inflammation, with popularization and application values.

The invention provides a method for producing a solution containing ²¹¹At⁻ (astatide ion) at a high radiochemical purity by using ²¹¹At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from ²¹¹At. The invention also provides a solution containing ²¹¹At⁻ (astatide ion) at a radiochemical purity of not less than 30%.