专利号:US-12410140-B2 优先权日:2020-06-19 标题:Method for synthesis of roxadustat and intermediate thereof, and intermediate thereof 发明人:ZHANG YONG; WANG GUO; YANG FEI; LIU FENGWEI; ZHOU CHUNDONG; ZHANG ZITONG 权利人:JUMPCAN SHANGHAI MEDICAL TECH CO LTD 摘要:Disclosed are a method for the synthesis of roxadustat and an intermediate thereof, and an intermediate thereof. In particular, disclosed is a method for the synthesis of compound M1, the method comprising the following steps: carrying out a reaction as shown below between compound SM and compound SM-A under the action of an oxidizing agent. The method of the present invention uses cheap and easily available raw materials, has short reaction steps, produces a high yield, has simple and convenient post-treatment procedures, and is suitable for industrial production.
专利号:WO-9502566-A1 优先权日:1993-07-16 标题 :Synthesis of combinatorial arrays of organic compounds through the use of multiple component combinatorial array syntheses 发明人:ARMSTRONG ROBERT W 权利人:UNIV CALIFORNIA; ARMSTRONG ROBERT W 摘要:The present invention relates to an array of compounds having a common core structure wherein the compounds of the array comprise the products of a multiple component combinatorial array synthesis having at least three components. The present invention also relates to the method of synthesizing that array. A further embodiment of the present invention relates to the use of solid phase synthesis to synthesize the combinatorial array of compounds. The present invention also relates to a method of creating a combinatorial array of compounds with a common core structure by identifying the desired core structure, identifying an MCCA reaction capable of generating that core structure, followed by preparing an array of compounds using the identified MCCA reaction according to the aforementioned method. The present invention also relates to a method for conducting in vitro assays of biological material using the combinatorial arrays of the present invention.
专利号:US-5419966-A 优先权日:1991-06-10 标 题 :Solid support for synthesis of 3'-tailed oligonucleotides 发明人:REED MICHAEL W; MEYER JR RICH B; PETRIE CHARLES R; TABONE JOHN C 权利人:MICROPROBE CORP 摘要:A solid support for oligonucleotide synthesis has the structure where CPG represents a controlled pore glass matrix, the wavy line represents a carbon chain covalently linking the NH group with the controlled pore glass matrix, X is 2,2'-dimethoxytrityl or H, and R is alkyl, aryl, arylalkyl, heteroalkyl, or heteroaryl. The dimethoxytrityl group is removed from the solid support by treatment with acid, and the oligonucleotide is built, step-by-step in a conventional synthesizer after attachment of the 3' end of the first oligonucleotide unit to the hydroxyl function connected to the R group.
专利号:US-2007173517-A1 优先权日:2006-01-20 标 题:Synthesis of 6,7-Dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides 发明人:WIRTH THOMAS; KROEBER JUTTA; NICOLA THOMAS; RAPP ARMIN; GUTHEIL DIETER; ORLICH SIMONE A; WANG XIAO-JUN; KRISHNAMURTHY DHILEEPKUMAR 权利人:WIRTH THOMAS; KROEBER JUTTA; NICOLA THOMAS; RAPP ARMIN; GUTHEIL DIETER; ORLICH SIMONE A; WANG XIAO-JUN; KRISHNAMURTHY DHILEEPKUMAR 摘要:Disclosed is an improved multi-step process for preparing a compound of Formula I: n n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
专利号:US-7737287-B2 优先权日:2002-03-28 标 题 :Anomeric derivatives of monosaccharides 发明人:MEUTERMANS WIM; WEST MICHAEL LEO; GIANG THANH LE; ADAMSON GEORGE; SCHAFER KARL; ABBENANTE GIOVANNI 权利人:ALCHEMIA LTD 摘要:This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.
专利号:US-7470795-B2 优先权日:2004-07-27 标 题:Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides 发明人:WANG XIAO-JUN; WIRTH THOMAS; NICOLA THOMAS; ZHANG LI; FRUTOS ROGELIO PEREZ; XU YIBO; KRISHNAMURTHY DHILEEPKUMAR; NUMMY LAURENCE JOHN; VARSOLONA RICHARD J; SENANAYAKE CHRIS HUGH; KROEBER JUTTA; REEVES DIANA 权利人:BOEHRINGER INGELHEIM PHARMA; BOEHRINGER INGELHEIM INT 摘要:Disclosed is a multi-step process for preparing a compound of Formula I: n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.