专利号:WO-2013018053-A1 优先权日:2011-08-02 标题 :Process for the preparation of epoxides as intermediates for the synthesis of nebivolol 发明人:CIPOLLONE AMALIA; D ANDREA PIERO; FATTORI DANIELA 权利人:MENARINI INT OPERATIONS LU SA; CIPOLLONE AMALIA; D ANDREA PIERO; FATTORI DANIELA 摘要:The present invention relates to a novel process of synthesis of epoxides, 6-fluoro-2- (oxiran-2-yl) chroman (Figure 1), intermediates for the synthesis of nebivolol, depicted in Scheme (1), enabling to obtain the above- mentioned epoxides in a racemic or semichiral form.
专利号:US-10392361-B2 优先权日:2016-01-21 标题:Process for the synthesis of intermediates of Nebivolol 发明人:BARTOLI SANDRA; MANNUCCI SERENA; GRISELLI ALESSIO; STEFANINI ALESSIO 权利人:MENARINI INT OPERATIONS LUXEMBOURG SA 摘要:The present invention relates to a novel process for the synthesis of the intermediate compounds constituted by chromanyl haloketones of formula III and 6-fluoro-2-(oxiran-2-yl)chromans of formula I. n The intermediates thus obtained can be used for the synthesis of Nebivolol.
专利号:US-8785664-B2 优先权日:2010-02-11 标 题 :Process for the preparation of nebivolol 发明人:BARTOLI SANDRA; CIPOLLONE AMALIA; FATTORI DANIELA 权利人:MENARINI INT OPERATIONS LU SA 摘要:The present invention relates to a novel process for the synthesis of Nebivolol product represented in Scheme (1), comprised of a reduced number of high-yield steps, and characterized by the kinetic resolution of the two epoxide pairs diastereoisomeric therebetween (mixture 1), allowing to avoid complex chromatographic separations.
专利号:US-8487122-B2 优先权日:2010-02-11 标题 :Process for the preparation of nebivolol 发明人:BARTOLI SANDRA; CIPOLLONE AMALIA; FATTORI DANIELA 权利人:BARTOLI SANDRA; CIPOLLONE AMALIA; FATTORI DANIELA; MENARINI INT OPERATIONS LU SA 摘要:The present invention relates to a novel process for the synthesis of Nebivolol product represented in Scheme (1), comprised of a reduced number of high-yield steps, and characterized by the kinetic resolution of the two epoxide pairs diastereoisomeric therebetween (mixture 1), allowing to avoid complex chromatographic separations.
专利号:US-2011250454-A1 优先权日:2010-04-09 标 题:Preparation of nebivolol 发明人:HALDAR PRANAB; GOLLA CHINA MALAKONDAIAH; SWAPNA AKULA; KUMAR KARRI VIJAYA; JAWLEKAR SUHAS; TUMMALA ARJUN KUMAR; PATRO DEEPALI; YARRAGUNTLA SESHA REDDY; RAMAKRISHNAN SRIVIDYA; CHIMALA VENKATA RAMANA REDDY 权利人:HALDAR PRANAB; GOLLA CHINA MALAKONDAIAH; SWAPNA AKULA; KUMAR KARRI VIJAYA; JAWLEKAR SUHAS; TUMMALA ARJUN KUMAR; PATRO DEEPALI; YARRAGUNTLA SESHA REDDY; RAMAKRISHNAN SRIVIDYA; CHIMALA VENKATA RAMANA REDDY 摘要:Processes for the synthesis of pharmacologically active 2,2-iminobisethanol derivatives, e.g., 2H-1-benzopyran-2 methanol-α,α′-iminobis(methylene)]bis-[6-fluoro-3,4-dihydro-[2R*[R*[R*(S*)]]]], and their pharmaceutically acceptable salts.
专利号:US-9090922-B2 优先权日:2010-11-30 标题:Process for the preparation of nebivolol 发明人:MAURO SANDRO; FATTORI DANIELA; D ANDREA PIERO; CIPOLLONE AMALIA; D ANDREA ENZO; ERCOLANO CARMELA 权利人:MAURO SANDRO; FATTORI DANIELA; D ANDREA PIERO; CIPOLLONE AMALIA; D ANDREA ENZO; ERCOLANO CARMELA; MENARINI INT OPERATIONS LU SA 摘要:The present invention relates to a novel process for the synthesis of the Nebivolol product depicted in Scheme 1, comprised of a reduced number of high-yield steps, and characterized by the enzymatic resolution of the chroman ester precursor.