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-2004249170-A1 优先权日:2002-01-24 标 题 :Process for preparing an intermediate useful for the asymmetric synthesis of duloxetine 发明人:BORGHESE ALFIO 摘要:This invention provides a process for the synthesis of(S)-3-Methylamino-1-2-thienyl)-1-propanol, a key intermediate in the synthesis of duloxetine.
专利号:US-5491243-A 优先权日:1993-10-12 标题 :Intermediate useful for the asymmetric synthesis of duloxetine 发明人:BERGLUND RICHARD A 权利人:LILLY CO ELI 摘要:This invention provides a stereospecific process for the synthesis of (S)-(+)-N,N-dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine, a key intermediate in the synthesis of duloxetine.
专利号:US-8192590-B1 优先权日:2008-04-14 标 题:Microwave-assisted formation of sulfonium photoacid generators 发明人:BELFIELD KEVIN D; YANEZ CICERON O 权利人:BELFIELD KEVIN D; YANEZ CICERON O; UNIV CENTRAL FLORIDA RES FOUND 摘要:Efficient method for preparing sulfonium photoacid generators (PAGs) by microwave-assisted reaction of diarylsufides in the presence of alkylaryliodonium salts. Microwave-assisted synthesis of the PAGs is significantly faster, reducing reaction time with less energy consumption. Reaction times using the microwave-assisted synthesis are in a range of from 90 to 420 faster than conventional thermal conditions. The photoacid quantum yields of several salts prepared by the microwave reaction were measured; the photoacid quantum yields of new sulfonium PAGs were in a range from 0.01 to 0.4 times greater than yields from conventional synthesis. Incorporating a nitro group in the structures of the sulfonium salts increased photoacid quantum yield, induced intersystem crossing and increased the efficiency of photoacid generation compounds.
专利号:US-2009076268-A1 优先权日:2007-09-14 标 题:Facile assembly of fused benzofuro-heterocycles 发明人:FITZGERALD ANNE E; LIU JING; MANI NEELAKANDHA S 权利人:FITZGERALD ANNE E; LIU JING; MANI NEELAKANDHA S 摘要:This invention concerns the synthesis of polycyclic structural components of pharmacological compounds, including the synthesis of fused benzofuro-heterocycles, through selective palladium-catalyzed cross-coupling and intramolecular cyclization.
专利号:US-2011281893-A1 优先权日:2010-05-11 标 题 :Compound, synthesis, composition and uses thereof 发明人:KANDULA MAHESH 权利人:KANDULA MAHESH; KRISANI BIOSCIENCES P LTD 摘要:The instant application provides the disclosure for a compound of formula I, synthesis of compound of formula I and its pharmaceutical acceptable salts, as well as its polymorphs, solvates, and hydrates thereof. The pharmaceutically acceptable salt may be formulated for oral administration, systemic administration, transdermal administration and injection. The compound of formula I and its pharmaceutical compositions may be used to treat cancer in mammal.
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合成参考文献
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