专利号:US-9453044-B2 优先权日:2012-02-07 标题 :Method of synthesizing peptides, proteins and bioconjugates 发明人:LIU CHUAN FA; ZHAO JUNFENG 权利人:UNIV NANYANG TECH 摘要:The invention relates to the synthesis of peptides, proteins and related bioconjugates, and in particular, to such synthesis using a peptide ligation method whereby a C-terminal salicylaldehyde ester peptide is reacted with an aminoacyl-N-hydroxl peptide. The invention also relates to the synthesis of cyclic peptides, including serinyl- or threonyl-containing cyclic peptides. The invention further relates to a solid phase synthesis of C-terminal salicylaldehyde ester peptides.
专利号:US-5714127-A 优先权日:1992-10-08 标题 :System for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J 权利人:WARNER LAMBERT CO 摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.
专利号:US-5702672-A 优先权日:1992-10-08 标 题 :Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KELL MICHAEL; PAVIA MICHAEL R; KIELY JOHN S; SCHROEDER MEL C; STANKOVIC CHARLES J; WARE STEVEN 权利人:WARNER LAMBERT CO 摘要:An apparatus for multiple, simultaneous synthesis of compounds which consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.
专利号:US-5766556-A 优先权日:1992-10-08 标题:Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA HELEN HOBBS; KIELY JOHN STEVEN; PAVIA MICHAEL RAYMOND; SCHROEDER MEL CONRAD; STANKOVIC CHARLES JOHN 权利人:WARNER LAMBERT CO 摘要:An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
专利号:US-5567391-A 优先权日:1992-10-08 标题 :Apparatus for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J 权利人:WARNER LAMBERT CO 摘要:An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
专利号:US-10669160-B2 优先权日:2018-04-30 标题:Heterogeneous wet synthesis process for preparation of high purity tungsten pentahalide 发明人:LIU YUMIN; LI FENG; WAN ZHIWEN; FAFARD CLAUDIA; WIESE STEFAN; HUSSON GUILLAUME; NIKIFOROV GRIGORY; SUI BIN; GIRARD JEAN-MARC 权利人:AIR LIQUIDE; AIR LIQUIDE AMERICAN 摘要:Synthesis of tungsten pentahalide compositions having low impurity profiles are disclosed. The specific impurity profile permits deposition of high purity tungsten-containing films using vapor deposition processes or other semiconductor manufacturing processes without introduction of performance-impacting contaminants.
参考标题:Studies On Hypolipidemic Agents. Ii Synthesis Of 1-Arenesulfonyloxy-2-Alkanone Derivatives As Potent Esterase Inhibitors And Hypolipidemic Agents. 作者:Kazuo Ogawa,Tadafumi Terada,Yoshiyuki Muranaka,Toshihiro Hamakawa,Sadao Hashimoto,Setsuro Fujii 摘要:Many 2-Oxoalkyl Arenesulfonate Derivatives Having Straight Or Branched Alkyl Chains Of Different Lengths, 2-Oxoalkyl Bis-Arenesulfonate Derivatives, And Alkyl Arenesulfonate Derivatives Having A Ketal Moiety At The 2-Position On The Alkyl Chain Were Synthesized, And Their Esterase-Inhibitory Activities, As Well As Hypolipidemic Activities, Were Evaluated.Among These Compounds, 1-(2, 4, 6-Trimethylbenzenesulfonyloxy)-2-Dodecanone (Iii-1U), And 1-(2, 3, 4, 6-Tetramethylbenzenesulfonyloxy)-2-Hexanone (Iii-1W), -2-Octanone (Iii-1X) And -2-Decanone (Iii-1Y) Exhibited Potent Esterase-Inhibitory Activities (Ic50=3X10-10, 2X10-10, 2X10<-10> And 3X<-11>M, Respectively). However, The Sulfonate (Xv) Having A Ketal Moiety On The Alkyl Chain And The Bis-Sulfonate (Xvi) Exhibited Low Inhibitory Activities Toward Esterase In Comparison With Iii And Xii. Most Of The Compounds Iii And Some Of The Compounds Xii Exhibited Potent Hypolipidemic Activities Corresponding To More Than 50% Lipid-Lowering Effect (Plasma Triglyceride And Cholesterol Ester) In Vivo. The Structure-Activity Relatioinships Of These Compounds Are Discussed.
合成参考文献
摘要:van Leeuwen, P. W. N. M., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 417. 摘要:Bronger, R. P. J.; Kamer, P. C. J.; Vogt, D., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 1, 32. 摘要:Compound: 1-Hexene, 4-methyl-, homopolymer