专利号:US-7247752-B2 优先权日:2004-10-01 标 题 :Methods for the synthesis of astaxanthin 发明人:LOCKWOOD SAMUEL F; TANG PENG CHO; NADOLSKI GEOFF; JACKSON HENRY L; FANG ZHIQIANG; DU YISHU; YANG MIN; GEISS WILLIAM; WILLIAMS RICHARD; BURDICK DAVID 权利人:CARDAX PHARMACEUTICALS INC 摘要:A method used for synthesizing intermediates for use in the synthesis of carotenoids and carotenoid analogs, and/or carotenoid derivatives. In some embodiments, the invention includes methods for synthesizing optically active intermediates useful for the synthesis of optically active carotenoids. Synthesis of optically active carotenoids, in one embodiment, may be accomplished by forming an optically active dihydroxy intermediate from ketoisopherone. The optically active dihydroxy intermediate may be converted into optically active astaxanthin derivatives.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-7692019-B2 优先权日:2000-12-04 标 题:Methods for the stereoselective synthesis of substituted piperidines 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
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-7858828-B2 优先权日:2008-03-26 标 题 :Process for synthesis of (3R,3'R,6'R)-lutein and its stereoisomers 发明人:KHACHIK FREDERICK; CHANG AN-NI 权利人:UNIV MARYLAND 摘要:(3R,3′R,6′R)-Lutein and (3R,3′R)-zeaxanthin are two dietary carotenoids that are present in most fruits and vegetables commonly consumed in the US. These carotenoids accumulate in the human plasma, major organs, and ocular tissues. In the past decade, numerous epidemiological and experimental studies have shown that lutein and zeaxanthin play an important role in the prevention of age-related macular degeneration (AMD) that is the leading cause of blindness in the U.S. and Western World. The invention provides a process for the synthesis of (3R,3′R,6′R)-lutein and its stereoisomers from commercially available (rac)-α-ionone by a C 15 +C 10 +C 15 coupling strategy. In addition, the present invention also provides access to the precursors of optically active carotenoids with 3-hydroxy-ε-end group that are otherwise difficult to synthesize. The process developed for the synthesis of lutein and its stereoisomers is straightforward and has potential for commercialization.
专利号:EP-1730108-B1 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin d analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.