专利号:US-6218542-B1 优先权日:1996-10-15 标 题:Synthesis of cisapride 发明人:DE KNAEP ALFONS GASTON MARIA; MOENS LUC JOZEF RAPHAEL; REY MAX 权利人:JENSSEN PHARMACEUTICA, N V 摘要:A new Process of preparing cisapride, and the pharmaceutically acceptable acid addition salts thereof, by reductively aminating 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinone in the presence of benzylamine under hydrogen in a reaction-inert solvent, yielding 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine having a cis/trans ratio of about 93/7, which is enriched in the amount of cis-stereoisomer by converting it into its acid addition salt, by treatment with a suitable inorganic acid, in an appropriate solvent, subsequent crystallisation and conversion to its free base form by treatment with an appropriate base, yielding 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine having a cis/trans ratio of equal to or higher than 98/2.
专利号:RU-2008112215-A 优先权日:2005-08-31 标 题 :METHODS OF SYNTHESIS AND INTERMEDIATE COMPOUNDS FOR THE SYNTHESIS OF STEREOISOMERIC COMPOUNDS SUITABLE FOR TREATMENT OF GASTROINTESTINAL DISORDERS AND DISORDERS OF THE CENTRAL NERVOUS SYSTEM
专利号:RU-2418798-C2 优先权日:2005-08-31 标 题 :Synthesis methods and intermediate compounds during synthesis of stereoisomeric compounds, suitable for treating gastrointestinal disorders and central nervous system disorders
专利号:US-7189852-B2 优先权日:2003-09-09 标题 :Synthesis 发明人:PALMER RICHARD MICHAEL JOHN; MEYERS NICHOLAS LESLIE; KNIGHT JOHN 权利人:ALIZYME THERAPEUTICS LTD 摘要:The present invention provides an improved process for the production of [(±)-endo]-4-amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride, compositions thereof, and intermediates thereto.
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:US-7427260-B2 优先权日:2001-03-30 标 题:Efficient methods for solid phase synthesis using trityl chloride resins 发明人:PANG YUAN-PING; PARK JEWN GIEW 权利人:MAYO FOUNDATION 摘要:Disclosed are efficient methods for loading amino derivatives onto trityl chloride resins and for cleaving chemically modified amino derivatives from trityl chloride resins. Methods for making a library of discrete chemically modified amino derivatives also disclosed.
摘要:Zhang, M.; Su, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 113. 摘要:Stewart, S. G., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 442. 参考文献:10.1248/cpb.50.941 摘要:Hirokawa Y, Harada H, Yoshikawa T, Yoshida N, Kato S. Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist. Chem Pharm Bull (Tokyo). 2002 Jul;50(7):941–59. doi: 10.1248/cpb.50.941.