CAS: 114870-03-0; (2S,3S,4R,5R,6R)-6-(((2R,3R,4R,5R,6R)-6-(((2R,3S,4S,5R,6R)-2-Carboxy-4-Hydroxy-6-(((2R,3S,4R,5R,6S)-4-Hydroxy-6-Methoxy-5-(Sulfoamino)-2-((Sulfooxy)Methyl)Tetrahydro-2H-Pyran-3-yl)Oxy)-5-(Sulfooxy)Tetrahydro-2H-Pyran-3-yl)Oxy)-5-(Sulfoamino)-4-(Sulfooxy)-

专利信息

专利号:WO-2022107013-A1
优先权日:2020-11-19
标 题 :Silver assisted gold catalysis for the preparation of fondaparinux pentasaccharide and intermediates
发明人：HOTHA SRINIVAS; WALKE GULAB; KASDEKAR NITESHLAL; SUTAR YOGESH
权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES
摘要:The present invention relates to a process for the synthesis of Fondaparinux pentasaccharide and its intermediates. Specifically, the present invention relates to a novel catalytic process for the synthesis of Fondaparinux pentasaccharide and its intermediates. The present invention further relates to a silver assisted gold catalysis for glycosylation reactions in the synthesis of Fondaparinux pentasaccharide and its intermediates. (I)

专利号:US-7655769-B2
优先权日:2004-07-20
标题:Orthogonally protected disaccharide building blocks for synthesis of heparin
发明人：HUNG SHANG-CHENG; LEE JING-CHYI; LU XIN-AN
权利人:ACADEMIA SINICA
摘要:Orthogonally protected disaccharide building blocks for synthesis of heparin saccharide are disclosed. The disaccharide building block has a formula (I), in which L is a leaving group, P 1 , P 2 , P 3 and P 4 are different, and of them P 1 is an ester-type protecting group, P 2 is a hydroxyl protecting group that could be oxidized to a carboxylic acid, P 3 is a hydroxyl protecting group, and P 4 is a hydroxyl protecting group which allows chemoselective deprotection with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). Acting as an elongation unit, the disaccharide building block of formula (I) may react with a starting unit of formula (II) to synthesize a heparin saccharide of desired size.

专利号:US-8822659-B2
优先权日:2008-10-08
标 题:Process for the synthesis of unprotected pentasaccharides from a protected pentasaccharide precursor
发明人：LOPEZ-BELMONTE ENCINA IVAN; OJEDA MARTINEZ DE CASTILLA RAFAEL
权利人:LOPEZ-BELMONTE ENCINA IVAN; OJEDA MARTINEZ DE CASTILLA RAFAEL; FARMACÉUTIOS ROVI S A LAB
摘要:Procedure for the synthesis of deprotected pentasaccharides from a protected precursor pentasaccharide through a reaction procedure having five stages whereamong is included an N-sulphation of amino groups and a hydrogenolysis of benzyl groups. Through this procedure a drastic reduction is achieved in the total synthesis time in comparison with the process traditionally employed, together with increased reproducibility thereof, permitting the standardization thereof.

专利号:US-11306157-B2
优先权日:2018-12-21
标 题:Expedient synthesis of core disaccharide building blocks from natural polysaccharides for heparan sulfate oligosaccharide assembly
发明人：HSIEH-WILSON LINDA C; PAWAR NITIN J; WANG LEI
权利人:CALIFORNIA INST OF TECHN
摘要:Methods for the preparation of oligosaccharide products from polysaccharide starting materials are disclosed. The methods include: hydrolyzing a glucosamine-containing polysaccharide starting material, such as heparin or heparosan, under conditions sufficient to form an oligosaccharide intermediate (e.g., a GlcN-IdoA disaccharide intermediate or a GlcA-GlcN disaccharide intermediate), and converting the oligosaccharide intermediate to the oligosaccharide product. Conversion of the oligosaccharide intermediates to the oligosaccharide products may include one or more esterification, acylation, epimerization, protection, and deprotection steps. Preparation of higher-order oligomers is described, as well as methods for selective oligosaccharide sulfation.

专利号:US-8987430-B2
优先权日:2009-10-30
标 题:Efficient and scalable process for the manufacture of fondaparinux sodium
发明人：PATEL PAYAL PARTH; MA CHUN; OHRR KEVIN K; NADJI SOURENA
权利人:PATEL PAYAL PARTH; MA CHUN; OHRR KEVIN K; NADJI SOURENA; RELIABLE BIOPHARMACEUTICAL CORP
摘要:The present invention relates to a process for the synthesis of the Factor Xa anticoagulent Fondaparinux and related compounds. The invention relates, in addition, to efficient and scalable processes for the synthesis of various intermediates useful in the synthesis of Fondaparinux and related compounds.

专利号:US-2014336369-A1
优先权日:2011-06-28
标题:Process for preparing heparinoids and intermediates useful in the synthesis thereof
发明人：KOVI RAVISHANKER; NAIK ASHISH; PATEL BRIJESH; MADALA MURALIKRISHNA
权利人:APICORE US LLC
摘要:Processes are disclosed for the synthesis of the Factor Xa anticoagulant fondaparinux and related compounds. Protected pentasaccharide intermediates and efficient and scalable processes for the industrial scale production of fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions are provided.