专利号:US-2015336866-A1 优先权日:2013-01-01 标题:Synthesis of difluoromethyl ethers and sulfides 发明人:HARTWIG JOHN; FIER PATRICK 权利人:UNIV CALIFORNIA 摘要:The synthesis of difluoromethyl ethers and sulfides with a simple, non-ozone-depleting reagent is described. The difluoromethylation of phenols with this reagent occurs at room temperature within minutes with exceptional functional group tolerance. The mild conditions makes possible tandem processes for the conversion of aryl boronic acids, aryl halides and arenes to difluoromethyl ethers. Mechanistic studies support a reaction pathway involving nucleophilic attack of the phenolate to difluorocarbene.
专利号:US-4161609-A 优先权日:1977-09-14 标题:Synthesis of carboxylic acid esters 发明人:CRAMER RICHARD D 权利人:DU PONT 摘要:A method is provided for converting a carboxylic acid amide to a carboxylic acid ester by reacting a vaporized mixture of the amide and an aliphatic alcohol or a phenol in the presence of a suitable catalyst at temperatures of from 100 DEG C. to 400 DEG C. The process is especially useful for the conversion of methacrylamide to methyl methacrylate.
专利号:US-2010056750-A1 优先权日:2006-12-21 标题:Process for the synthesis of halogenated aromatic diacids 发明人:RITTER JOACHIM C 权利人:RITTER JOACHIM C 摘要:The production of high-purity halogenated aromatic diacids from halogenated dimethylbenzene by oxidation with an oxygen-containing gas is conducted using a four-component catalyst system and a two-stage temperature process.
专利号:US-9820979-B2 优先权日:2011-07-13 标 题:FXR (NR1H4) binding and activity modulating compounds 发明人:KINZEL OLAF; STEENECK CHRISTOPH; KREMOSER CLAUS 权利人:GILEAD SCIENCES INC 摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:US-9580409-B2 优先权日:2011-11-07 标 题:Modulators of opioid receptors and methods of use thereof 发明人:MALCOLM SCOTT; BOWEN CARRIE; MELNICK LAURENCE; XIE LINGHONG 权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., μ-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-9676721-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.