424results about "Isotope introduction to organic compounds" patented technology

New microfluidic devices, useful for carrying out chemical reactions, are provided. The devices are adapted for on-chip solvent exchange, chemical processes requiring multiple chemical reactions, and rapid concentration of reagents.

Provided is an organic electroluminescent device that exhibits an efficient host-dopant energy transfer mechanism, and thus, expresses a certain high-efficiency electroluminescent performance, based on improved electron density distribution. The organic electroluminescent device also overcomes low initial efficiency and short operation life property, and secures high-performance electroluminescent performance with high efficiency and long life property for each color.

The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.The compounds of this invention have formula I or II:wherein the variables are as defined herein.

The present invention provides improved radioiodinated phospholipid ether analogs which demonstrate significant tumor avidity and longer plasma half-life than shorter-chain analogs. The radioiodinated phospholipid ether analogs of the present invention provide superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.

Positron emitting compounds and methods of their production are provided. The compounds have the formula: (F)m G (R)n wherein each R is a group comprising at least one carbon, nitrogen, phosphorus or sulfur atom and G is joined to R through said carbon, nitrogen, phosphorus or sulfur atom; G is silicon or boron; m is 2 to 5 and n is 1 to 3 with m+n=3 to 6 when G is silicon; m is 1 to 3 and n is 1 to 3 with m+n=3 to 4 when G is boron; and wherein the compound further comprises one or more counterions when the above formula is charged; and wherein at least one F is 18 F.

Improved radioiodinated phospholipid ether analogs are described which exhibit significant tumor avidity and longer plasma half-life relative to shorter chain analogs. Use of these compounds results in superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.

Tellurium (Te)-containing precursors, Te containing chalcogenide phase change materials are disclosed in the specification. A method of making Te containing chalcogenide phase change materials using ALD, CVD or cyclic CVD process is also disclosed in the specification in which at least one of the disclosed tellurium (Te)-containing precursors is introduced to the process.

Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and / or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and / or premature ejaculation are described.

In one aspect, the present invention provides a method for labeling a terminal olefin, the method comprising a step of treating a terminal olefin substrate having the structure: with a labeled ethylene reagent in the presence of a suitable catalyst under suitable olefin metathesis reaction conditions to form a labeled terminal olefin having the structure: wherein RA and RB are independently hydrogen, or an aliphatic, alicyclic, heteroaliphatic, heterocyclic, aryl or heteroaryl moiety, with the proviso that RA and RB are not each hydrogen, or RA and RB taken together with the carbon atom to which they are attached form an alicyclic or heterocyclic moiety; and * denotes the presence of an isotopic label on the terminal carbon atom.

Methods and compositions utilizing ether and alkyl phospholipid ether analog compounds for treating cancer and imaging, monitoring, and detecting cancer stem cells in humans.

Methods and apparatus enable radiosynthesis of radiolabeled compounds using electrochemical trapping and release. The trapping and release of radioactive isotopes all occur inside a microreactor, a vial or similar device, thus eliminating the need for azeotropic drying and several dead-end filling steps, as well as the necessity to move concentrated radioisotopes from one compartment of the chip to another. These and other features allow radioisotope enrichment to be carried out internally within a radiochemical synthesis chip, providing faster and more robust operation, as well as producing very high radiochemical labeling yields.

New microfluidic devices, useful for carrying out chemical reactions, are provided. The devices are adapted for on-chip solvent exchange, chemical processes requiring multiple chemical reactions, and rapid concentration of reagents.

The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.

The present invention provides a method for preparing [F-18]-fluoride ion which comprises the step of bringing [O-18]-enriched water containing [F-18]-fluoride ion formed by proton irradiation of [O-18]-enriched water into contact with a strongly acidic cation exchange resin to remove impurity cations, the step of then bringing the [O-18]-enriched water containing [F-18]-fluoride ion treated above into contact with a weakly basic anion exchange resin to make [F-18]-fluoride ion adsorbed to the resin and, along therewith, to recover the [O-18]-enriched water which has passed through the resin, and the step of eluting and collecting the [F-18]-fluoride ion adsorbed to the weakly basic anion exchange resin. According to the method for preparing [F-18]-fluoride ion of the present invention, [F-18]-fluoride ion can be collected at a high collection efficiency even from a larger amount (about 2 ml or more) of [O-18]-enriched water containing [F-18]-fluoride ion than the amount in prior method, and moreover expensive [O-18]-enriched water can be recovered and reused in the preparation of [F-18]-fluoride ion.

The invention provides a diaminopyrimidine compound and a composition containing the same and discloses the diaminopyrimidine compound shown as in a formula (I) and a drug combination containing the compound or salt thereof acceptable in crystal form and pharmacy, hydrate or solvent complex, stereoisomer, pro-drug or isotope variant. The diaminopyrimidine compound and the composition containing the same have excellent inhibition effect on protein kinase and have better pharmacokinetic parameter characteristics, and drug concentration of the compound in animal bodies can be increased to improve drug efficacy and safety.

The present invention relates to amino acids, complexes, and compounds comprising deuterium and tritium isotopes preferably alpha deuterated amino acids, polypeptides, antibodies, derivatives and saccharide-amino acid complexes and conjugates. In some embodiments, the invention relates to methods of using compounds comprising deuterium for imaging biochemical concentrations and distributions in mammalian tissues using nuclear magnetic resonance spectroscopy. In some embodiments, the invention relates to the used of said amino acids derivatives and complexes in boron neutron capture therapy. In some embodiments, the present invention relates to the preparation of amino acids, polypeptides, antibodies, derivatives and saccharide complexes / conjugates comprising heavy hydrogen isotopes. In some embodiments, the invention relates to racemizing amino acids starting from compositions of any optical purity. In further embodiments, the invention relates to the preparation of amino acids and their N-acyl counterparts with deuterium incorporated at the alpha carbon.

A method for producing a compound having a deuterated aromatic ring or heterocyclic ring according to the invention includes heating a compound having an aromatic ring or heterocyclic ring in the presence of heavy water, a transition metal and a metal which generates deuterium. As the metal which generates deuterium, at least one metal selected from the group consisting of aluminum, magnesium, zinc, iron, lead and tin is preferred. As the transition metal, at least one metal selected from the group consisting of platinum, palladium, ruthenium and rhodium is preferred. The heating is preferably carried out by microwave irradiation.

A method for obtaining a halogenated organic compound, whereby an organotrifluoroborate compound is reacted with a halide ion in the presence of an oxidizing agent to produce the corresponding halogenated organic compound. The method may be used for producing radiohalogenated organic compounds.

A carbon hydrogen structure (C: H) is one of the basic structures in the pharmaceutical chemistry structure and a formed C-H bond is the basic chemical bond. The invention discloses a preparation method and an application of deuterated drugs which can change the chemical bond energy and the hydrogen bond energy in the structure of pharmaceutical compound. The hydrogen atom (H) in pharmaceutical compound structure is substituted by the A deuterium atom (D) which is the isotope of hydrogen, therefore changing the molecular structure and the bond energy of the substituted pharmaceutical compound so as to form a new deuterated drug. The deuterated drugs can be used for pharmacokinetics research, can obviously enhance the disease-preventing or treating function of the drugs, and can reduce the toxic and side effect of the drugs.

The present invention relates to methods of eluting radionuclide-labeled or radionuclide-labeled compounds using solid phase extraction resins, devices for carrying out such methods and computer programs for controlling such devices. In particular, the method of the invention enables the automated synthesis of radionuclide-labeled compounds using anion-exchange resins or reversed-phase resins, and involves removing or eluting the anion-exchange resin-bound The step of radionuclide labeling (fluorine-18, etc.) or a radionuclide-labeled compound bound to a reversed-phase resin.

The present invention relates to an apparatus for synthesizing F-18 labeled radioactive pharmaceutical. The apparatus for synthesizing F-18 labeled radioactive pharmaceutical includes an F-18 radioactive isotope supplier, a reagent supplier, a polymer precursor cartridge, a first heating unit, a polymer compound cartridge, a synthesizing container, a second heating unit, a water liquid container, a transmitting gas supplier, a cleansing liquid supplier, a connection tube, a plurality of control valves, and a controller.

The invention relates to a method for preparing deuterated diphenyl urea. Specifically, the invention provides an intermediate N-(1, 1, 1-3 deuterated methyl) benzo succinimide which can be used for preparing a deuterated diphenyl urea compound and an application of the intermediate in the preparation of the deuterated diphenyl urea compound. The method can be used for conveniently preparing the intermediate with the high purity and various deuterated diphenyl urea compounds in high efficiency.

The invention provides a method for the synthesis of an 18F-labelled product comprising deprotected of a protected 18F-labelled compound using a deprotection agent comprising a weak acid and wherein neutralisation and buffering of the deprotected product are carried out by the addition of a neutralisation agent. The deprotected product is buffered in a pH range suitable for subsequent autoclaving and formulation into an injectable radiopharmaceutical.

A process for producing a radioactive fluorine compound which comprises a step in which [18O] water containing [18F] fluoride ions is introduced into a column packed with an ion-exchange resin to collect the [18F] fluoride ions and a step in which a substrate is reacted with the [18F] fluoride ions collected, characterized in that the ion-exchange resin is a resin represented by the following general formula (1): (wherein n is an integer of 1 to 10; R represents a linear or branched, C1-8 monovalent hydrocarbon group; P represents a styrene-based copolymer; and Y represents an anion).

The invention provides a small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer and relates to an automatic PET drug synthesizer. The small modular multifunctional automatic 18F labelling PET drug synthesizer comprises a single FDG (fluorodeoxyglucose) synthesis module or two FDG synthesis modules which are connected in series, namely a module FDG1 and a module FDG2, a PET drug product separating system and a control system, wherein the single FDG synthesis module or the two FDG synthesis modules which are connected in series are used for independently completing FDG synthesis or continuously completing double-batch FDG synthesis in a combined manner; the PET drug product separating system is connected with the single FDG synthesis module or a second module, namely the module FDG2, in the two FDG synthesis modules which are connected in series; and the control system is used for connecting and controlling the FDG synthesis module and the PET drug product separating system. The small modular multifunctional automatic PET drug synthesizer has the characteristics of ingenious structure, small size, simple mounting, friendly interface, simple operation, safety, stability, reliability, convenience in maintenance, powerful function and flexibility, is simple to mount and operate, and convenient to maintain, and the production requirement of 18F labelling PET drugs for the current market and scientific research can be met.

The invention relates to the technology of microscale reactor, in particular to a microscale reactor for synthesizing radioactive drug. The microscale reactor is composed of a sealing-in body, a reaction flask, a separation column and an adsorption column, wherein the sealing-in body is sealed by a fluid channel layer, a middle layer and a control channel layer into a whole; the reaction flask, the separation column and the adsorption column are detachably spliced into the sealing-in body. The fluid passage layer comprises a fluid microchannel which causes fluid to communicate with each reaction flask, the separation column and the adsorption column; the control channel layer comprises a control air microchannel and an air chamber corresponding to the fluid microchannel; a microvalve is composed of an air chamber and a middle layer to control the fluid microchannel to open and close. The microfluidic chip of the invention can synthesize common positron nuclide of microscale volume. The invention has simple and easy preparation technology method, needs no expensive equipment, can reduce space and invested capital for protecting equipment for preparing radioactive drug and can reduce the workload of experimenters.

The invention relates to a synthesis method of a stable isotope-labeled beta receptor agonist type compound. The synthesis method comprises the following steps: (1) by taking stable isotope-labeled methanol as a raw material, reacting with acetone or stable isotope-labeled acetone, and ammonifying to obtain stable isotope-labeled tert-butylamine; and (2) by taking a bromoketone type compound as a precursor of the beta receptor agonist type compound, reacting with stable isotope-labeled tert-butylamine to prepare the stable isotope-labeled beta receptor agonist type compound. Compared with the prior art, the method for preparing the stable isotope-labeled beta receptor agonist, provided by the invention, is simple, safe and reliable, the chemical purity of the product after separation and purification is above 99.0%, the isotopic abundance is above 98.0% atom, and the product can fully meet the requirements of residual detection in the field of food safety.

The invention provides a method for preparing a deuterated aromatic organic compound. The method comprises the following steps: firstly, dissolving a halogenated aromatic compound and an alkali metal salt MA into a deuterated solvent or a mixed solvent of the deuterated solvent and a common solvent, dropping an organic silicon reagent, performing stirring reaction at minus 40 DEG C to 150 DEG C, and performing separation purification after reaction, thereby obtaining the deuterated aromatic organic compound. By adopting the method, the deuterated aromatic organic compound can be efficiently, economically and environment-friendly prepared without participation of a transition metal or a metallic tin reagent, and the deuteration rate of the prepared deuterated product is greater than 95%. The method is gentle in condition, good in substrate universality and high in yield, and the prepared deuterated compound can be widely applied to fields of medicine chemistry and organic chemistry.