45results about How to "High radiochemical yield" patented technology

The invention provides a fluorine-18-marked pyridazinone analogue. The general structural formula of the analogue is shown as a formula (A), wherein G is selected from S, O or NH; R1 is alkyl with 1-6 carbon atoms; R2 is halogen or halogenation alkyl; L is phenyl, cyclohexyl or a hexa-heterocycle radical containing heteroatoms; m is 1, 2, 3, 4, 5 or 6; n is an integer of 1-15; and M is methylene or ethoxy. A compound marking method is simple, and has high radiation chemistry yield, high stability, a high myocardium initial uptake value, high target to non-target ratio and low using cost. The pyridazinone analogue is applied to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine as a novel fluorine-18-marked myocardial perfusion developing agent.

The invention discloses an 18F-labeled compound and a pod protease targeted PET imaging probe, which relates to the technical fields of radiopharmaceuticals and nuclear medicine. The invention provides a compound shown as a formula (I), asparagine site shearing and disulfide bond reduction are carried out in a tumor microenvironment with high expression of pod protease, and a radioactive dimer 18F-1-dimer is formed by virtue of a biocompatible CBT-Cys click condensation reaction, so that the tumor imaging effect is improved. The compound with a structure shown in the formula (I) is synthesizedby adopting a one-step ion exchange 18F labeling method, the method is simple to operate, and preparative HPLC for further purification is not needed. The invention further provides the pod proteasetargeted PET imaging probe which is a compound shown in (I). The PET imaging probe has the advantages of high stability, high sensitivity, strong specificity, good safety and the like.

The present invention relates to the field of medicinal chemistry, and in particular relates to 18F-labeled ethinyloestradiol and a preparation method and application thereof, a modifying group is introduced into ethinylestradiol, and the ethinylestradiol is labeled by 18F, and the 18F-labeled ethinyloestradiol has good bioactivity, excellent pharmacokinetic properties and good stability in vitro, can be better targeting to breast cancer ER + cells, and can be used as a PET tracer for early diagnosis or therapeutic effect evaluation of high metastatic breast cancer ER + cells. The invention also provides the preparation method of the 18F labeled ethinylestradiol, a labeling group is introduced into the ethinylestradiol as a raw material by Click reaction, and heated for being exchanged with 18F<-> under relatively mild conditions, a labeling step and purification time are simplified, the radiochemical yield of the 18F-labeled ethinyloestradiol is high, and commercial application and clinical promotion of radiolabeled compounds are facilitated.

Provided herein is a one-step method for chelating actinium-225 to a construct comprising a chelator linked to a bio-molecule, such as, an antibody or monoclonal antibody, via a bifunctional ligand in, for example, a 3-arm configuration. Also provided are methods for increasing the radiochemical yield of an actinium-225-chelant-biomolecule complex and for producing a high specific activity actinium-225 complex. The chelation is performed at a physiological temperature, about 37° C. Also provided are high specific activity actinium-225 complexes, that is, actinium-225 chelated to the chelator-biomolecule construct and pharmaceutical compositions thereof. Further provided are methods of treating a neoplastic disease or disorder with the actinium-225 complexes.

The present disclosure, among other things, provides new technologies for preparation of medical isotope labeled metal(loid) chalcogen nanoparticles for use in medical imaging and/or therapeutic applications. Provided technologies show a number of advantages as compared with previously available options for preparing and utilizing medical isotopes, including, for example, they utilize metal(loid) chalcogen nanoparticles that serve as universal binders (e.g., via covalent or non-covalent (e.g., chelate) bonds) for medical isotopes to provide medical isotope labeled metal(loid) chalcogen nanoparticles. Surprisingly, the same metal(loid) chalcogen nanoparticles may be used to bind (e.g., covalent or non-covalent e.g., chelation) bonding) a wide variety of different useful medical isotopes without the use of traditional chelating agents.

The invention discloses a class of iodine radioisotope labeled benzyl phenyl ether derivatives, a preparation method, a pharmaceutical composition and application thereof, and specifically relates toa benzyl phenyl ether derivative represented by a general formula I, a pharmaceutical salt, a stereoisomer and a preparation method thereof, a composition containing one or more radioactive compounds,and application of the radioactive compounds as PD-L1 tracers in human or animal bodies in diagnosis and treatment of diseases related to PD-1/PD-L1 signaling pathways, such as cancer, infectious diseases and autoimmune diseases.

The invention provides an anilinoquinazoline compound, namely a quinazolinyl-4-anilino-2-(N,N,N-trialkyl) quaternary ammonium salt derivative, which is synthesized into a 2-[fluorine-18]fluoro substituted derivative through the radiochemistry and used as a fluorine-18 labeled precursor, and can be applied to the preparation of a tumor positron imaging agent; the tumor positron imaging agent adopts an epidermal growth factor as a target spot and can perform imaging of a specific tumor. According to the invention, the preparation method for the derivative has the following advantages: the synthesis steps are simple, and the target compound can be obtained at only one step that the quaternary ammonium salt precursor is labeled by the fluorine-18; the time for radiochemical synthesis is short, and only 20-25 min is required; the separation is simple and convenient without adopting HPLC, the product of which the radiochemical purity is more than 98 percent can be obtained with one Sep-Pak C-18 column, and meanwhile the quaternary ammonium salt precursor is removed; the radiochemical yield is high, the non-correction yield can reach 40-60 percent, and the drug specific radioactivity is high. The structural formula is shown in the specification.

A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes and 4-haloethenylphenyl tropane families are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter protein with high affinity and selectivity. The invention provides methods of synthesis which incorporate radioisotopic halogens at a last step which permit high radiochemical yield and maximum usable product life. The radiolabeled compounds of the invention are useful as imaging agents for visualizing the location and density of serotonin transporter by PET and SPECT imaging.

Disclosed are an [¹⁸F]fluoromethyl group-introduced radiotracer for brain neuroinflammation-targeting positron emission tomography (PET), the synthesis thereof, and a method for evaluating biological results using the same. In the method for the synthesis of an [¹⁸F]fluoromethyl group-introduced radiotracer for brain neuroinflammation-targeting positron emission tomography, a compound obtained by introducing triazolium triflate into normethyl-PBR28 is used as a precursor and a fluoromethyl group is labeled with fluorine-18 in a single step. The [¹⁸F]fluoromethyl group-introduced radiotracer for brain neuroinflammation-targeting positron emission tomography is synthesized by using a compound, obtained by introducing triazolium triflate into normethyl-PBR28, as a precursor and performing substitution with fluorine-18 in a single step.

The invention relates to a fluorinated phosphine oxide compound used in the preparation of a positron emission imaging agent and a preparation method thereof, and has a structure shown in a formula I.For the first time, fluorinated phosphine oxide is used as an 18F-labeled auxiliary group, a positron nuclides probe is constructed by a 18F-19F isotope exchange strategy, a labeling method is mild in conditions, reactions can be directly conducted in an 18F-aqueous solution without blow-drying 18F-, and the compound has high radiochemical yield, easy purification, no need for high performance liquid chromatography separation and purification and broad application prospects in the field of positron drugs of preparing biomolecules such as heat sensitive and solvent sensitive peptides or proteins and the like.

The invention discloses 18F click labelling transferrin receptor targeting polypeptide T7 as well as a preparation method and application thereof. According to the preparation method, synthesis steps of click chemistry are improved, addition amount of a prosthetic group TsOTEGay is reduced, the addition amount of polypeptide T7 is appropriately increased, feeding ratio of the prosthetic group to the polypeptide T7 is adjusted to be 1:(1-2); after 18F-TEGay is synthesized through reaction, a polypeptide precursor is directly added for carrying out click reaction without carrying out HPLC purification, a 'one-pot two-step' process is adopted for synthesizing 18F-TEG-T7, and finally HPLC purification is carried out; and one purification process is reduced, the whole synthesis and purification time is greatly reduced and can be controlled to be within 120 minutes, radiochemical yield is about 28.26 minus and plus 7.43% (n=3). The optimized 'two-step one-pot' click reaction can be applied to research of 18F labelling polypeptide, and a novel tumor targeted probe can be prepared.

The invention relates to a synthetic strategy of using perfluoro crown ethers and other macrocycles to bind to [18F]-labelled fluorination reactions. The optional use of implementing perfluoro kryptofix 2.2.2 in this process is also disclosed. The present invention also claims perfluoro kryptofix structures that are suitable for use in 18F-labelling of fluorous based structures.

The invention discloses a <18>F-labeled-8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene (S14161) and a preparation method thereof. The preparation method has the following advantages: preparation raw materials are cheap and are easy to obtain, the synthesis process is simple, reaction conditions are mild, and the radiochemical synthesis time is short; the above product is simple and convenient to purify and separate, the radiochemical purity of the product exceeds 98%, the radiochemical yield of the product is high, the uncorrected yield reaches up to 92%, and the radioactivity of the product is high; and the product is useful in the inspection and diagnosis of tumors and the radiation therapy of the tumors. The structural formula of the <18>F-labeled-8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene is shown in the description.

Disclosed is a method for producing precursors for L-3,4-dihydroxy-6-[¹⁸F]fluorophenylalanine and 2-[¹⁸F]fluoro-L-tyrosine and the α-methylated derivatives thereof, the precursor, and to a method for producing L-3,4-dihydroxy-6[¹⁸F]fluorophenylalanine and 2-[¹⁸F]fluoro-L-tyrosine and the α-methylated derivatives thereof from the precursor. A compound of formula (3) is provided which enables automated synthesis of L-3,4-dihydroxy-6-[¹⁸F]fluorophenylalanine and 2-[¹⁸F]fluoro-L-tyrosine. The enantiomeric purity of the product is ≧98%.

The invention discloses a quinazoline compound and a preparation method and application thereof. The quinazoline compound as a medical developer has stable structure and high developing resolution. The preparation method is simple to perform, has short reaction time and high radioactive chemical yield and is easy to apply to industrial large-scale production.

The invention belongs to the field of radioactive medicine labeling, and in particular to an activatable tumor apoptosis PET (positron emission computed tomography) developer, as well as a preparationmethod and application thereof. The activatable tumor apoptosis PET developer has a structure as shown in a formula (I), the labeling process only needs 30 minutes, the labeling time is short, the radiochemical yield of the labeling product can reach 54 percent, the specific activity is 1.2 Ci/umol, the radiochemical purity is more than 98 percent, the labeling efficiency is high, the stability is high and the preparation steps are simple. The labeling product has high in-vitro stability, has high targeting property on apoptotic cells, can serves as a PET developer to detect tumor apoptosis,and also can be applied to early diagnosis of related diseases caused by abnormal cell apoptosis, detection progress, early curative effect evaluation after treatment or development of new treatment schemes and personalized diagnosis and treatment schemes.