专利号:US-6258323-B1 优先权日:1998-11-16 标题:Apparatus and method used in multiple, simultaneous synthesis of general compounds 发明人:HORMANN ROBERT EUGENE; GILBERT DARYL EUGENE; SIOMA EDWARD MICHAEL 权利人:ROHM & HAAS 摘要:The apparatus and method of the present invention provides for conducting simultaneous multiple synthesis of general compounds, which often takes place under varied uneven conditions requiring heating, cooling, agitation, reagent/solvent additions to the reactor contents at each reaction vessel location, supply and maintenance of inert atmosphere and means to facilitate the reflux of the reactor contents. Thus, it becomes necessary to monitor and control the reaction conditions during the simultaneous multiple synthesis of general compounds. The apparatus allows the user to connect various independently controlling and conveying means to each reaction vessel through multiple ports provided on a stopper mounted on each reaction vessel. The apparatus of the present invention permits user to readily access the reaction vessels without interrupting the reactions occurring in the adjacent reaction vessels. The unique geometry and shape of the stopper allows positioning of multiple ports, while still providing the stopper with a compact size. As a result, a large array of reaction vessels can be accommodated in the device of the present invention without significantly increasing the overall size of the apparatus. Some of the general compounds that can be readily synthesized by the apparatus and the method of the present invention include inorganic compounds as well as organic compounds, such as oligomers, polymers, agricultural chemicals, drugs, peptides and oligonucleotides.
专利号:WO-9611194-A1 优先权日:1994-10-06 标题:Pyridonecarboxylic acid derivative and intermediate for the synthesis of the same 发明人:OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 权利人:DAINIPPON PHARMACEUTICAL CO; OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 摘要:A pyridonecarboxylic acid derivative represented by general formula (I), an ester and a salt thereof, an antibacterial agent containing the same, and a bicyclic amine compound serving as a direct intermediate for the synthesis of the pyridonecarboxylic acid derivative, wherein R represents cycloalkyl, optionally substituted phenyl, etc.; G represents carbon, etc.; A represents C-Z (Z being hydrogen, halogeno, lower alkoxy, etc.) or nitrogen; X represents hydrogen, amino, etc.; Y represents hydrogen or halogeno; m is an integer of 1 to 3; and W represents -(CH2)nN(R1)R2 (R1 and R2 being the same or different and each representing hydrogen, lower alkyl, etc., and n being an integer of 0 or 1).
专利号:US-6017911-A 优先权日:1996-02-27 标 题 :Pyridonecarboxylic acid derivatives and intermediates for the synthesis thereof 发明人:HORIUCHI NOBUHIKO; YONEZAWA TAKENORI; CHIBA KATSUMI; YOSHIDA HIROAKI 权利人:DAINIPPON PHARMACEUTICAL CO 摘要:This invention relates to pyridonecarboxylic acid derivatives of the following general formula, esters thereof and salts thereof, as well as pharmaceutical preparations containing them. ##STR1## wherein: R is cycloalkyl which may be substituted by halogen, or the like; n X is hydrogen, lower alkyl, amino or the like; n Y is hydrogen or halogen; n A is nitrogen or a group of the formula C--Z in which Z is lower alkoxy that may be substituted by halogen, or the like; n R 1 and R 2 may be the same or different and are each hydrogen or the like; n R 3 is hydrogen or lower alkyl; n R 4 , R 5 , R 6 , R 7 , R 8 and R 9 may be the same or different and are each hydrogen, halogen or lower alkyl; n m is 0 or 1; and n n and p may be the same or different and are each 0 or 1. n This invention also relates to bicyclic amine compounds useful as direct intermediates for the synthesis of the above-described pyridonecarboxylic acid derivatives.
专利号:US-6841559-B1 优先权日:1999-11-19 标 题:Pyridinones to treat and prevent bacterial infections 发明人:ALMQVIST FREDERIC; EMTENAS HANS; HULTGREN SCOTT J; PINKNER JEROME S 权利人:WASHINGTON UNIVERSITY OF ST LO 摘要:Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:WO-9601260-A1 优先权日:1994-07-01 标题 :Pyridonecarboxylic acid derivative, ester thereof, salt thereof, and intermediate for synthesis of these compounds 发明人:FUJITA MASAHIRO; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 权利人:DAINIPPON PHARMACEUTICAL CO; FUJITA MASAHIRO; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 摘要:A pyridonecarboxylic acid derivative represented by general formula (I), an ester thereof, a salt thereof, and an antibacterial containing these compounds, wherein R represents optionally halogenated cycloalkyl, optionally substituted phenyl, etc.; G represents carbon, etc.; A represents C-Z or nitrogen; Z represents hydrogen, halogen, lower alkoxy, halogenated lower alkoxy, lower alkyl, halogenated lower alkyl, lower alkoxy-lower alkyl, etc.; X represents hydrogen, halogen, optionally protected amino, lower alkyl, etc.; Y represents hydrogen or halogen; R1 and R2 represent each independently hydrogen, lower alkyl, etc.; R3 represents hydrogen, halogen, lower alkoxy, lower alkoxy-lower alkyl, halogenated lower alkyl, etc.; and n represents an integer of 0 or 1. The invention also relates to a bicyclic amine compound as a direct intermediate for the pyridonecarboxylic acid derivatives.
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合成参考文献
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