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-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:US-4751312-A 优先权日:1984-07-20 标 题:Process and intermediates for the synthesis of diastereomeric compounds 发明人:GASTEIGER JOHANN; KAUFMANN KARLHEINZ; MENGEL RUDOLF 权利人:BAYER AG 摘要:A new process for the controlled synthesis of the two diasteromeric forms of triazolyl-O,N-acetals of the formula (I) in which R represents optionally substituted phenyl, optionally substituted phenoxy, optionally substituted alkoxy, optionally substituted alkoxy, optionally substituted alkylthio, alkylcarbonyl, nitro or halogen and n represents an integer from 0 to 5, with the proviso that R can represent identical or different radicals, if n represents an integer from 2 to 5. New trans-substituted oxiranes and their use as intermediates for the synthesis of compounds of the formula (I).
专利号:EP-1709057-B1 优先权日:2004-01-21 标 题:Synthesis of spongosine 发明人:OUZMAN JACQUELINE VALERIE ANNE 权利人:CAMBRIDGE BIOTECHNOLOGY LTD 摘要:Reaction of 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose with 2-methoxyadenine to form 9-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-2-methoxyadenine, then deprotection of the 9-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-2-methoxyadenine to form spongosine is described. Synthesis of intermediates for use in the synthesis of spongosine is also described.
专利号:US-8742028-B2 优先权日:2009-05-06 标 题:Solid support for Fmoc-solid phase synthesis of peptide acids 发明人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R 权利人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R; MALLINCKRODT LLC 摘要:The present invention provides a solid support for Fmoc-solid phase synthesis of peptides. In particular, the solid supports of the invention may be utilized to produce peptide acids.
专利号:US-8420848-B2 优先权日:2009-01-09 标题:Process for the synthesis of beta glycerol phosphate 发明人:KULKARNI YASHWANT 权利人:KULKARNI YASHWANT; SIGMA ALDRICH CO LLC 摘要:The present invention provides methods for the preparation of beta glycerol phosphate and its salts. In particular, the invention provides efficient methods for the synthesis of beta glycerol phosphate of high purity.
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合成参考文献
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