66results 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.

The subject invention relates to the compositions for radiolabeling Diethylenetriaminepentaacetic Acid (DTPA)-dextran with Technetium-99m and for stabilizing the DTPA-dextran Cold Kit. The composition contains Stannous Chloride ions to reduce 99mTc-pertechnetate, Ascorbic Acid to reduce stannic ions to stannous ions to maintain a reducing environment, α,α-Trehalose to add bulk and to stabilize the lyophilized composition without interfering with the radiochemical yield, and Glycine to transchelate Technetium-99m under highly acidic conditions to facilitate radiolabeling DTPA-dextran with high radiochemical purity. In addition, the invention pertains to methods for making and using the compositions. The reconstitution of the lyophilized composition by 99mTc-pertechnetate, resulting in radiolabeled 99mTc-DTPA-dextran in a composition between pH 3 to 4. This invention contains a Diluent vial, which when used will shift the pH to a moderately acidic pH, which would provide less pain on injection and ease-of-use to clinical practioners for adjusting its potency.

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 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 discloses a technetium-99m-labelled colchicine complex, a preparation method thereof and a purpose thereof. The preparation method is characterized in that trimethyl colchicum acid and DTPA acid anhydride are subjected to coupling and hydrolysis to obtain a novel ligand DTPA-CHC, the ligand is subjected to <99m>Tc direct labeling under reducing action of stannous to obtain the technetium-99m-labelled colchicine complex, complex radiochemical purity is greater than 90%, the complex exists at room temperature for more than 6 h in a stable mode, and lipid-water partition coefficients determination shows that <99m>Tc-DTPA-CHC is a water-soluble compound. The technetium-99m-labelled colchicine complex has good tumor ingestion and detention effects, tumor / muscle ratio is high, tumor imaging is clear, and the technetium-99m-labelled colchicine complex can be used for SPECT imaging diagnosis for tumor.

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 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 losing 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 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 discloses a technetium-99m labelled Melphalan complex as well as a preparation method and application thereof. The preparation method is characterized by coupling and hydrolyzing Melphalan and DTPA (diethylenetriaminepentaacetic acid) anhydride to obtain a novel ligand DTPA-MFL, and then carrying out <99m>Tc direct labelling on the ligand under the stannous reducing action, thus obtaining the technetium-99m labelled Melphalan complex. The Melphalan complex has the beneficial effects that the radiochemical purity of the complex is more than 90%; the complex can stably exist at room temperature for more than 6 hours; and water partition coefficient determination indicates that the complex is a water-soluble compound. The technetium-99m labelled Melphalan complex has good tumor uptake and retention and tumor / muscle ratio, is clearer in tumor imaging and can be used for SPECT (single-photon emission computed tomography) imaging diagnosis of tumors.

The invention discloses high-specific-activity tritium-labeled zaltoprofen and a preparation method thereof, and belongs to the technical field of medicine preparation. According to the method, 2-(3-carboxymethyl-4-phenylthiophenyl)methyl propionate is used as a raw material, and is subjected to three-step reaction of bromine substitution, dehydration condensation and hydrolysis to generate 4-bromo zaltoprofen, the 4-bromo zaltoprofen and tritium gas are subjected to tritium-halogen exchange under the actions of a palladium-carbon catalyst and an alkali acceptor to prepare 4-<3>H-zaltoprofen,and the synthesized product is subjected to preparation liquid phase purification to obtain tritium-labeled zaltoprofen with high specific activity (29.30 ci / g), high radiochemical purity (greater than or equal to 98%) and high chemical purity (greater than or equal to 99%). According to the invention, the prepared 4-<3>H-zaltoprofen provides a material basis for researching the absorption, distribution, metabolism and excretion of zaltoprofen in an animal body.

The invention provides a preparation method of technetium labeled pyrroloquinoline quinone dimethyl ester, belonging to the fields of biotechnology and medicine. By the preparation method, the structure of pyrroloquinoline quinone (PQQ) is modified, and PQQ-Z is prepared; and 99mTc labeling is carried out, and 99mTc-PQQ-Z is prepared. The product 99mTc-PQQ-Z has high radiochemical purity; and compared with the 99mTc-PQQ, the lipid / water partition coefficient of the 99mTc-PQQ-Z is increased from 1.49 to 0.67, the electrical property of the 99mTc-PQQ-Z is changed from anion electrical property to electric neutrality, and the brain entering amount of the 99mTc-PQQ-Z is twice of that of the 99mTc-PQQ.

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 relates to a method for preparing 131I-metaiodobenzylguanidine with high radioactive specific activity and without a carrier. The method comprises the following steps: performing normal-temperature reaction on a labeled precursor N,N'-di(t-butyloxycarboryl)-3-(tributyltin)-bethanidine, a buffer solution, an oxidizing agent and Na131I for 20 minutes, and adding a reducing agent and heating to 100 DEG C to react for 20 minutes; standing after the reaction is finished, cooling to room temperature, adding anion exchange resin and lightly stirring for 2 minutes; absorbing supernate and passing through a microfiltration membrane to obtain the product. The 131I-metaiodobenzylguanidine, prepared by using hydrogen peroxide--trifluoroacetic acid or N-chlorosuccinimide--sodium pyrosulfite as the oxidizing agent and the reducing agent, has high radiochemical purity and high radioactive specific activity. Reaction byproducts are removed from the 131I-metaiodobenzylguanidine solution after anion exchange resin treatment and microfiltration membrane filtration, and the tin amount is reduced to trace amount, so the 131I-labeled metaiodobenzylguanidine is suitable for clinical diagnosis and treatment. The condition of the labeling reaction is mild and simple, so preparation can be finished in a hospital, and high cost and decay loss of medicines caused by transportation are avoided.

The invention provides a tetrahydroxy furfuryl piperazine compound bonded with a sigma-1 receptor and a preparation method and application of the compound. The structural formula of the compound is shown as the formula (I) (please see the formula I in the description), wherein R is F, 18F, I or OCH2CH2F. The ligand compound of the tetrahydroxy furfuryl piperazine sigma-1 receptor has proper affinity and selectivity for the sigma-1 receptor and is one of few sigma-1 receptor ligands with nanomole-scale affinity and low fat solubility. When the R group in the compound of the formula (I) is 18F, 18 F is marked in two steps through p-fluorine[18F]benzaldehyde. The compound has high marking rate, high radiochemical purity and excellent biological property, can be applied to a PET developing tracer agent, and has wide clinical application prospects.

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 carbon-11 labeled Larotrectinib compound, the chemical structural formula of the compound is as follows: the compound can be obtained by mixing and reacting with carbon-11 labeled fluorophosgene, or the compound can be obtained by introducing carbon-11 labeled carbon dioxide into a solution containing BEMP and then adding POCl3 after the reaction is finished, and the compound is obtained by reacting with the BEMP and the POCl3. Compared with the prior art, the synthesis of the short half-life period carbon-11 labeled Larotrectinib is successfully realized, the radiochemical purity of the marker is high, and the short half-life period carbon-11 labeled Larotrectinib is suitable for clinical requirements on the short half-life period carbon-11 labeled Larotrectinib.

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 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.