专利号:US-9708317-B2 优先权日:2013-11-25 标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives 发明人:ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY 权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL 摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
专利号:US-2024024489-A1 优先权日:2020-11-20 标 题:Protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof 发明人:MULARD LAURENCE; DHARA DEBASHIS; PFISTER HELENE; PAOLETTI JULIE; PHALIPON ARMELLE; GUERREIRO-INVERNO CATHERINE 权利人:PASTEUR INSTITUT 摘要:The present invention provides zwitterionic oligosaccharides, in particular fragments of the surface polysaccharides from Shigella sonnei and Shigella sonnei conjugates comprising them. The present invention also provides protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof, the disaccharide repeating unit of Shigella sonnei being: (I)
专利号:WO-9939201-A1 优先权日:1998-02-03 标 题 :SOLUTION AND SOLID PHASE SULFOXIDE GLYCOSYLATION: SYNTHESIS OF β-LINKED OLIGOSACCHARIDES USING 2-DEOXY-2-N-TRIFLUOROACETAMIDO-GLYCOPYRANOSYL DONORS 发明人:SILVA DOMINGOS; SOFIA MICHAEL J 权利人:INTERCARDIA RESEARCH LAB INC 摘要:The invention relates to a process for the synthesis of β-oligosaccharides. β-oligosaccharides are synthesized using alkylsulfenyl- or an arylsulfenyl-2-deoxy-2-N-trifluoroacetamidoglycopyranoses as glycosyl donors via the sulfoxide glycosylation, both in solution and solid phases. Once activated under the glycosylation conditions, these donors afford the respective β-glycosides exclusively and in high yield. Since the trifluoroacetamido group is easily removed under mild conditions, the corresponding amino group can be appropriately derivatized, even in the presence of unprotected hydroxyl groups. Disaccharide libraries are designed, constructed and analyzed. The invention also relates to a process for synthesizing the glycosyl donor.
专利号:US-10899773-B2 优先权日:2014-12-19 标 题 :Total synthesis of trioxacarcin DC-45-A2 and preparation of trioxacarcin analogs 发明人:NICOLAOU KYRIACOS C; CAI QUAN 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
专利号:US-9428524-B2 优先权日:2010-05-25 标 题:Synthetic process for the manufacture of ecteinascidin compounds 发明人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN 权利人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN; PHARMA MAR SA 摘要:This invention relates to compounds of formula II: wherein R 1 , R 2 , Prot SH , and Prot NH are as defined, to processes for the synthesis of ecteinascidins of formula I from compounds of formula II, and to processes for the synthesis of compounds of formula II.
专利号:US-2014323705-A1 优先权日:2011-05-13 标题:Manufacture of lacto-n-tetraose 发明人:HEDEROS MARKUS; DEKANY GYULA; DEMKÓ SÃ?NDOR; Kovács Imre; BAJZA ISTVÃ?N 权利人:HEDEROS MARKUS; DEKANY GYULA; DEMKÓ SÃ?NDOR; Kovács Imre; BAJZA ISTVÃ?N 摘要:The present invention relates to the synthesis of the tetrasaccharide of formula (I) and novel intermediates used in the synthesis.
[参考文献]: Cheng-Yang Huang, Et Al. Effect Of Metal Binding And Posttranslational Lysine Carboxylation On The Activity Of Recombinant Hydantoinase. J Biol Inorg Chem. 2009 Jan;14(1):111-21.
合成参考文献
摘要:Rodríguez-Morgade, M. S.; Torres, T., Science of Synthesis Knowledge Updates, (2017) 2, 67.