子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 181 | System for purification and analysis of radiochemical products yielded by microfluidic synthesis devices | US11895636 | 2007-08-23 | US07741121B2 | 2010-06-22 | Arkadij M Elizarov; Hartmuth C. Kolb; Jianzhong Zhang |
| The present application is generally directed to microfluidic devices and methods for the achievement and assessment of chemical and radiochemical purity of (microfluidic) radio-synthesis products. More particularly, the current application relates to systems for purification and analysis of radiochemical products yielded by microfluidic synthesis devices. | ||||||
| 182 | Method of deprotection | US11576625 | 2005-09-23 | US07714115B2 | 2010-05-11 | Julian Grigg; Nigel Osborn |
| 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. | ||||||
| 183 | NONFLOW-THROUGH APPRATUS AND MEHOD USING ENHANCED FLOW MECHANISMS | US12578175 | 2009-10-13 | US20100093098A1 | 2010-04-15 | Carroll Edward Ball; Arkadij Elizarov; Hartmuth C. Kolb |
| Methods and apparatus for facilitating the synthesis of compounds in a nonflow-through device are presented. Application of the nonflow-through methods and microfluidic devices to the synthesis of radiolabeled compounds is described. These methods and apparatus enable the introduction of a pressurized gas through a tangential slit into a vortex reactor of the nonflow-through device, while one or more liquids are delivered to the reaction chamber through the same or different inlet ports. The introduction of the pressurized gas produces a cyclonic motion of the mixture within the reactor. Such a mechanism may be used to facilitate the evaporation of various liquids within the reactor at lower temperatures, thus reducing the production of unwanted byproducts that are associated with the use of high temperatures. In addition, thorough mixing of various liquids may be effected rapidly while allowing chemical reactions to take place efficiently within the vortex reactor. | ||||||
| 184 | Catalytic radiofluorination | US11065345 | 2005-02-24 | US07632485B2 | 2009-12-15 | David R. Elmaleh; Alan J. Fischman; Timothy M. Shoup |
| One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal. | ||||||
| 185 | MINIATURIZED LIQUID SURFACE REACTIONS USING NANOMOLAR AMOUNTS OF CONCENTRATED [11C]CARBON DIOXIDE IN A STATIONARY GAS-PHASE | US12158712 | 2006-12-19 | US20090092549A1 | 2009-04-09 | Tor Kihlberg; Bengt Langstrom |
| Methods and reagents for miniaturized carboxylation with carbon-isotope labeled carbon dioxide using Grignard reagents or other organometallic reagents in a closable reaction loop or reactor are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals or precursors for radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided. | ||||||
| 186 | ISOTOPICALLY TAGGED SYNONS FROM 2 CARBON PRECURSORS | US12035871 | 2008-02-22 | US20080269527A1 | 2008-10-30 | Rodolfo A. Martinez |
| The use of vinyl sulfides, sulfoxides and sulfones in synthetic chemistry for the production of a wide variety of materials is well known. For example, phenyl vinyl sulfides, sulfoxides and sulfones have been used for the synthesis of important heterocycles, in combinatorial chemistry and as Diels-Alder adducts. Although these compounds have been used extensively for a variety of applications, the isotopically labeled versions have not been reported. A simple route for the isotopically labeled production of these important building blocks has been developed. | ||||||
| 187 | Method of Deuteration Using Mixed Catalyst | US10585629 | 2004-12-21 | US20080234488A1 | 2008-09-25 | Nobuhiro Ito; Tsuneaki Maesawa; Kazushige Muto; Kosaku Hirota; Hironao Sajiki |
| The subject of the present invention is to provide a method for deuteration, which can obtain a compound having an aromatic ring and/or a heterocyclic ring at an improved deuteration ratio. The present invention relates to a method for deuteration of a compound having an aromatic ring and/or a heterocyclic ring, comprising reacting the compound having an aromatic ring and/or a heterocyclic ring with a heavy hydrogen source in the presence of an activated mixed catalyst of not less than two kinds of catalysts selected from among a palladium catalyst, a platinum catalyst, a rhodium catalyst, an iridium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst. | ||||||
| 188 | Methods and Apparatus for Production and Use of [11C] Carbon Monoxide in Labeling Synthesis | US11571631 | 2005-07-08 | US20080095693A1 | 2008-04-24 | Tor Kihlberg; Bengt Langstrom; Tommy Ferm; Jonas Erikson |
| Methods and apparatus for production and use of carbon-isotope monoxide in labeling synthesis are provided. The resultant carbon-isotope labeled reagents are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided | ||||||
| 189 | Method and apparatus for synthesis of [11c] phosgen using concentrated [11c] carbon monoxide with uv light | US10581835 | 2004-11-29 | US20070110664A1 | 2007-05-17 | Tor Kihlberg; Tommy Ferm; Bengt Langstrom |
| Methods and systems for labeling synthesis of phosgen by UV light are provided. Methods of synthesizing labeled compounds useful as PET tracers from labeled phosgen are also provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography. Associated kits for PET studies are also provided. | ||||||
| 190 | Radical trap in fluoridation of iodonium salt | US10559879 | 2004-12-17 | US20060292060A1 | 2006-12-28 | Harry Wadsworth; David Widdowson; Emmanuelle Wilson; Michael Carroll |
| Decomposition of iodonium salts by a free radical process has been identified as a significant factor in the observed yield variability of fluoridation reactions using said iodonium salts. Accordingly, the inclusion of a free radical trap in the reaction mixture blocks the radical chain decomposition pathway for iodonium salts such that only the reaction leading to fluoridation can occur and the yield of aryl fluoride becomes high and reproducible. The reaction may also be carried out on solid phase. In both the solution and the solid phase the preferred method of the present invention is radiofluoridation. | ||||||
| 191 | Methods of [11c]-radiolabelling phenothiazine and phenothiazine-like compounds | US10573882 | 2004-09-27 | US20060275209A1 | 2006-12-07 | Lutz Schweiger; Stuart Craib; Andrew Welch; Peter Sharp |
| This invention pertains to methods of [11C]-radiolabelling “phenothiazine” and “phenothiazine-like” compounds, which have a pendant group (which is a primary amino group; a cationic primary imino group; a secondary amino group; a cationic secondary imino group; a primary imino group; or a secondary imino group), by reaction with [11C]methyl trifluoromethanesulfonate (CF3SO2O11CH3), also known as [11C]methyl triflate. This reaction converts the pendant group into a [11C]methyl-labelled pendant group. The resulting [11C]-radiolabelling product is useful, for example, as an in vivo positron emission tomography (PET) tracer, for example, for patients suffering from melanoma, the most serious form of skin cancer, and tauopathy (e.g., Alzheimer's disease). The present invention also pertains to the resulting [11C]-radiolabelling products, compositions comprising them, their use in methods of (e.g., PET) imaging, their use in methods of medical treatment and diagnosis, etc. | ||||||
| 192 | Fluorous labeling for selective processing of biologically-derived samples | US10544609 | 2004-11-12 | US20060263886A1 | 2006-11-23 | Eric Peters; Scott Brittain; Ansgar Brock; Scott Ficarro; Arthur Salomon |
| This invention provides fluorous-based methods and compositions for preparation, separation and analysis of complex biologically-derived samples, such as proteomic and metabolomic samples. | ||||||
| 193 | Polymer precursors of radiolabeled compounds, and methods of making and using the same | US10091168 | 2002-03-04 | US07018610B2 | 2006-03-28 | Duncan H. Hunter; Mustafa Janabi |
| One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds. | ||||||
| 194 | Reagents and methods for labeling terminal olefins | US10929624 | 2004-08-30 | US20060045846A1 | 2006-03-02 | Thomas Horstmann; Bryan Lewis |
| 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. | ||||||
| 195 | Methods for carbon isotope labeling synthesis by transition metal-promoted carbonylation via isocyanate using azides and carbon-isotope monoxide | US11086632 | 2005-03-22 | US20060002851A1 | 2006-01-05 | Bengt Langstrom; Julien Barletta; Hisashi Doi; Masaaki Suzuki; Ryoji Noyori; Yasuyoshi Watanabe; Farhad Karimi |
| Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided. | ||||||
| 196 | Process for deuteration of inert methylene | US10516638 | 2002-11-12 | US20050177015A1 | 2005-08-11 | Kosaku Hirota; Hironao Sajiki |
| The present invention relates to a method for deuteration of an inert alkane using activated palladium carbon. The present invention discloses “A method for deuteration of a hydrogen atom of a methyl group or a hydrogen atom bonded to a carbon atom at benzyl position and the other carbon atoms of an alkylene group having not less than 2 carbon atoms, in a compound containing the methyl group or the-alkylene group having not less than 2 carbon atoms, directly bonded to an aromatic ring which may have a substituent, which comprises placing said compound in a deuterated solvent in the presence of activated palladium carbon, under sealed reflux condition”. | ||||||
| 197 | Methods for purifying radiolabelled compounds | US10686950 | 2003-10-16 | US20040260073A1 | 2004-12-23 | John F. Valliant; Peter N. Dorff; Raman Chirakal |
| One aspect of the present invention relates to a method of purifying radiolabelled compounds comprising a) loading onto a fluorous polymer a radiolabelled compound precursor comprising a fluoroalkyl tin moiety; b) reacting the radiolabelled compound precursor with a radiolabel delivering compound to give a radiolabelled compound, wherein the fluoroalkyl tin moiety is replaced by a radiolabel; and c) eluting the radiolabelled compound from the fluorous polymer. | ||||||
| 198 | Solid-phase nucleophilic fluorination | US10482540 | 2004-07-15 | US20040236085A1 | 2004-11-25 | Sajinder Kaur Luthra; Frank Brady; Harry John Wadsworth; Alexander Mark Gibson; Matthias Eberhard Glaser |
| The present invention relates to novel solid-phase processes for the production of radiolabelled tracers, in particular for the production of 18F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers. The invention also comprises radiopharmaceutical kits using these novel processes. | ||||||
| 199 | Statement regarding federally sponsored research or development | US10854375 | 2004-05-25 | US20040225121A1 | 2004-11-11 | Robert C. Bergman; Steven R. Klei |
| A process for labeling organic compounds with deuterium and tritium is described using specific catalysts. | ||||||
| 200 | Solid-phase electrophilic fluorination | US10482542 | 2003-12-24 | US20040186312A1 | 2004-09-23 | Sajinder Kaur Luthra; Frank Brady; Harry John Wadsworth |
| The invention relates to compounds of formula (I); wherein R1 and R2 independently selected from C1-6 alkyl; P1, P2, P3, and P4 are each independently hydrogen or a protecting group; and their use in the preparation of 18F-labelled 6-L-fluorodopa. 1 | ||||||
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