专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
专利号:US-6184168-B1 优先权日:1997-09-22 标题:Synthesis of 1,4-trans-polybutadiene using a lanthanide organic acid salt catalyst 发明人:LYNCH THOMAS J 权利人:BRIDGESTONE CORP 摘要:The invention provides a catalyst composition, comprising: (a) an organolithium compound; and, (b) an organic acid salt of lanthanide series element; wherein: (1) only components (a) and (b) are required to promote the synthesis of 1,4-trans-polybutadiene; (2) the ratio of component (a) to component (b) is selected to maximize formation of the trans structure of said 1,4-trans-polybutadiene; and, (3) components (a) and (b) are selected for enabling further diblock synthesis. The invention further contemplates a process for using the catalyst to synthesize 1,4-trans-polybutadiene and other polymers and copolymers having trans configuration in the conjugated diene monomer contributed units.
专利号:US-2008086013-A1 优先权日:2006-06-15 标 题:Carbometallation of alkynes and improved synthesis of uniquinones 发明人:LIPSHUTZ BRUCE H 权利人:UNIV CALIFORNIA 摘要:Methods for the carbometallation of alkynes are presented. Those are useful for the synthesis of CoQ 10 and other ubiquinones as well as for the synthesis of ubiquinol analogs.
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-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
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