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-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-9815771-B2 优先权日:2014-08-06 标题 :Method for the synthesis of mirabegron and its derivatives 发明人:MARQUILLAS OLONDRIZ FRANCISCO; RIEGO ARBOLEYA ESTELA 权利人:INTERQUIM SA 摘要:The present invention refers to a method for the synthesis of a compound of formula (I), solvates, stereoisomers or salts thereof, a key intermediate in the synthesis of Mirabegron by reduction of an amide in the presence of an amine-boranecomplex, wherein the amine is an aniline.
专利号:EP-2644590-A1 优先权日:2012-03-30 标 题:Synthesis of 2-(3,4-difluorophenyl)cyclopropanamine derivatives and salts 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
专利号:US-8093436-B2 优先权日:2008-03-19 标题 :Process for synthesis of (3R,3′R)-zeaxanthin and (3R,3′S;meso)-zeaxanthin from (3R,3′R,6′R)-lutein via (3R)-3′,4′-anhydrolutein 发明人:KHACHIK FREDERICK 权利人:KHACHIK FREDERICK; 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 and accumulate in the human plasma, major organs, and ocular tissues. Another stereoisomer of (3R,3′R)-zeaxanthin that is not of dietary origin but is found in the human ocular tissues is (3R,3′S;meso)-zeaxanthin. There is growing evidence that these carotenoids 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 the Western World. In view of the potential therapeutic application of dietary lutein, (3R,3′R)-zeaxanthin, and (3R,3′S;meso)-zeaxanthin, the industrial production of these carotenoids is of considerable importance. The present invention provides a process for the partial synthesis of (3R,3′R)-zeaxanthin and (3R,3′S;meso)-zeaxanthin from a readily accessible dehydration product of (3R,3′R,6′R)-lutein, namely, (3R)-3′,4′-didehydro-β,β-caroten-3-ol [(3R)-3′,4′-anhydrolutein]. The process involves regioselective hydroboration of (3R)-3′,4′-anhydrolutein to a mixture of (3R,3′R)-zeaxanthin and (3R,3′S;meso)-zeaxanthin followed by separation of these carotenoids by enzyme-mediated acylation.
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.