专利号:US-2004138469-A1 优先权日:2002-12-23 标 题 :Process for the synthesis of torsemide, in particular of pure and stable form II 发明人:LUSSANA MASSIMILIANO; RAINONI MAURO; GAMBUZZA FILIPPO 权利人:COSMA S P A 摘要:The present invention relates to a new process for the synthesis of torsemide, in particular of pure and stable form II, which comprises direct synthesis of torsemide from 4-(3-methylphenylamino)-3-pyridine-sulphonamide. The new process envisages fewer steps than the processes described in the prior art, with improved yields and good quality from the chemical and preferably polymorphous points of view.
专利号:US-6399820-B2 优先权日:1998-11-04 标题:Process and reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function 发明人:DESMURS JEAN-ROGER; MILLET ANDRE; PEVERE VIRGINIE 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.
专利号:US-4105651-A 优先权日:1976-03-15 标 题:Purification of enkephalin, an endogenous composition in the human body and synthesis of same 发明人:HUGHES JOHN 权利人:US HEALTH EDUCATION & WELFARE 摘要:The purification of an endogenous composition isolated from mammalian brain tissue and termed enkephalin ('in the head'). Enkephalin is recovered from brain tissue by acetone solution and purified by means of column and thin layer chromatography. The composition which is a mixture of two pentapeptides, namely, (a) H-Tyr-Gly-Gly-Phe-Met-OH and (b) H-Tyr-Gly-Gly-Phe-Leu-OH wherein the ratio of a:b is from 3:1 to 4:1 has been found to be a non-addictive narcotic and an opiate agonist. n The synthesis of the pentapeptide composition from the known structure above is accomplished by conventional solution techniques of protection of the amino groups, such as t-butyloxycarbonyl, benzyloxycarbonyl, and t-amyloxycarbonyl, or the solid phase peptide synthesis of R. Bruce Merrifield using a polymeric support and the same or similar amine protecting groups.
专利号:US-10768157-B2 优先权日:2015-10-20 标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples 发明人:KABIR ABUZAR; FURTON KENNETH G 权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.
专利号:US-7279572-B2 优先权日:2003-05-22 标题:Process for the 2-stage synthesis of hexanitrohexaazaisowurtzitane starting from a primary amine 发明人:CAGNON GUY; ECK GENEVIEVE; HERVE GREGOIRE; JACOB GUY 权利人:SNPE MATERIAUX ENERGETIQUES 摘要:A subject-matter of the present invention is a novel process for the synthesis of hexanitrohexaazaisowurtzitane (HNIW), a compound of use as energetic filler in powders, propellants and explosives. n This process comprises a first stage of reaction of an α,β-dicarbonyl derivative with a primary amine which makes it possible to form a hexasubstituted hexaazaisowurtzitane derivative. n The HNIW is subsequently obtained directly, in a single reaction stage, by nitration of the hexasubstituted hexaazaisowurtzitane derivative. n This process, in only 2 stages starting from a primary amine, is particularly simple and inexpensive.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.