专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-8063062-B2 优先权日:2006-12-20 标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL 权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV 摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.
专利号:US-2009177008-A1 优先权日:2005-12-28 标题:Novel process for synthesis of itopride and its novel intermediate n-(4-hydroxybenzyl)- 3,4-dimethoxybenzamide 发明人:KHAMAR BAKULESH MAFATLAL; MODI INDRAVADAN AMBALAL; VENKATRAMAN JAYARAMAN; RAVI PONNAIAH; NORI DIVAKARA SOMAYAJULU; GAJULA MADHUSUDANA RAO; RENUGADEVI GURUSAMY; SHASHIKALA KUNJARU N; RUDRAMUNI SANTOSH M 权利人:CADILA PHARMACEUTICALS LTD 摘要:The present invention relates to a novel and improved process for the preparation of N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide—known as Itopride, via a novel intermediate N-(4Ëœhydroxybenzyl)-3,4-dimethoxybenzamide.
专利号:US-12024483-B2 优先权日:2019-11-13 标题 :Synthesis method of hydroxybenzylamine 发明人:XU CHANGPING; JIA YANRONG 权利人:TAIZHOU CHUANGYUAN INDUSTRIAL TECH CO LTD 摘要:The present invention relates to a synthesis method of hydroxybenzylamine, belonging to the technical field of organic synthesis. The principle of the method is a demethylation reaction of methoxybenzylamine in the presence of hydrobromic acid. The present invention has the characteristics that methoxybenzylamine and hydrobromic acid are distilled at reflux to remove redundant water to improve a reaction temperature and increase the concentration of hydrobromic acid in a reaction mixture, thereby enhancing the demethylation of hydrobromic acid on methoxybenzylamine and then shortening a reaction time and increasing a conversion rate; when generation of a methyl bromide gas is not observed, distillation is continued, excess hydrobromic acid is recycled to further improve the reaction temperature and increase the conversion rate and meanwhile reduce the consumption of raw material hydrobromic acid and decrease the processing capacity of the subsequent steps and the consumption of raw material sodium hydroxide.
专利号:US-2025259704-A1 优先权日:2022-06-24 标 题:Systems and methods for cell-free iterative site saturation mutagenesis and its application for the directed evolution of enzymes catalyzing unnatural reactions 发明人:JEWETT MICAHEL C; BOGART JONATHAN W; LANDWEHR GRANT M; Karim Ashty Stephen 权利人:UNIV NORTHWESTERN 摘要:Disclosed are methods, compositions, systems, and protein compounds for the directed evolution of enzymes and proteins. The method comprising generating variant protein with a desired functionality, comprising one or more DNA expression templates comprising nucleic acid sequences encoding a variant protein, expressing the variant protein using cell-free protein synthesis; and analyzing one or more parameters associated with the variant protein.
专利号:WO-2007074386-A3 优先权日:2005-12-28 标题:A novel process for synthesis of itopride and it’s novel intermediate-n-(4-hydroxybenzyl)-3,4-dimethoxybenzamide
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