专利号:US-2015239796-A1 优先权日:2014-02-19 标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane 发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS 权利人:UNIV OSLO 摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).
专利号:US-2009264680-A1 优先权日:2004-07-07 标题:Process for the synthesis and purification of (4-methoxybutyl) (4-trifluoromethylphenyl) methanone 发明人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 权利人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 摘要:A process for the preparation of 4-trifluoromethylvalerophenone is described. The process described is a three step process comprising the synthesis of organomagnesium specie, coupling reaction between the organomagnesium specie and trifluoromethylbenzonitrile or trifluoromethylbenzoyl chloride and preferably a purification of the product obtained in suitable reaction conditions. In the process an extraction phase of the final product is not required.
专利号:US-4822903-A 优先权日:1981-05-15 标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof 发明人:JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT 权利人:RHONE POULENC SPEC CHIM 摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.
专利号:US-6380436-B1 优先权日:1998-05-12 标 题 :Process for the synthesis of alkoxyalkyl (trifluormethylphenyl) methanones 发明人:THENNATI RAJAMANNAR; DEO KESHAV; MIDHA AJAY SOHANLAL; CHANDRA TILAK; PATEL VIJAY MULJIHHAI 权利人:SUN PHARMACEUTICAL IND LTD 摘要:A new process is described for the preparation of (alkoxyalkyl)(4-trifluoromethylphenyl)methanones. The process comprises reacting a 4-trifluoromethylbenzonitrile with an alkoxyalkyl Grignard in the presence of a suitable polar aprotic solvent. The compound (4-methoxybutyl)(4-trifluoromethylphenyl)methanone is useful as an intermediate in the preparation of the antidepressant drug fluvoxamine.
专利号:WO-2008084057-A1 优先权日:2007-01-10 标题:Compounds with a combination of cannabinoid-cb1 antagonism and serotonin reuptake inhibition 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G 权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G 摘要:This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.
专利号:US-5254558-A 优先权日:1991-08-15 标 题:Substituted 1,3-diazines as leukocyte elastase inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ICI PLC 摘要:The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.