专利号:US-8785629-B2 优先权日:2009-06-18 标题 :Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability 发明人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO 权利人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO; CENTRE NAT RECH SCIENT; UNIV ORLEANS 摘要:Synthons for the synthesis of phosphonates prodrugs POM and POC, especially for direct Cross Metathesis.
专利号:WO-2014148928-A1 优先权日:2013-03-21 标 题:Method for incorporating protecting acetal and acetal ester groups, and its application for the protection of hydroxyl function 发明人:MARKIEWICZ WOJCIECH; TOÅš-MARCINIAK AGNIESZKA; CHMIELEWSKI MARCIN 权利人:INST CHEMII BIOORG POLSKIEJ AKADEMII NAUK 摘要:The present invention is the method for incorporation of acetal and acetal ester groups for protection of hydroxyl function. The method is applied in particular in the processes of RNA synthesis. The method can be employed in the synthesis of nucleosides with acetal and acetal ester groups for the protection of hydroxyl functions. The method according to the invention consists of the reaction of an organic compound containing at least one hydroxyl group, soluble in an aprotic solvent, with a compound of the general formula 1, R 1 -S-CH 2 -O-R 2 (1) in the presence of SnCl 4 , in an aprotic solvent. In the second aspect, the present invention is the method of protecting the hydroxyl function, particularly in position 2', in nucleoside derivatives, based on the incorporation of an acetal or acetal ester group.
专利号:US-8536318-B2 优先权日:2008-05-29 标题 :Chemical RNA synthesis method 发明人:DEBART FRANCOISE; VASSEUR JEAN-JACQUES; LAVERGNE THOMAS 权利人:DEBART FRANCOISE; VASSEUR JEAN-JACQUES; LAVERGNE THOMAS; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER 2 摘要:The invention relates to a method for the chemical synthesis of RNA, comprising the following steps: a) bonding to a solid support of a monomer having formula (II) in which—X 1 is a dimethoxytrityl group,—X 6 is H or an OAc group or OX 3 , in which X 3 is a group having formula (A), in which X is O or S, R′ is H or CH 3 and R is selected from a linear or branched alkyl group at C 1 to C 4 and a R 1 —O—R 2 group in which R 1 is an alkyl group at C 1 to C 2 and R 2 is a CH 3 group or CH 2 CH 2 —O—CH 3 or aryl; b) assembly with the monomer having formula (II) bound to the support thereof obtained in step (a) of at least one monomer having formula (III) in which X 1 , Bp, X 3 are as defined for formula (II) and X 5 is a hydrogen phosphonate monoester or phosphoramidite group, preferably a 2-cyanoethyl-N,N-diisopropylphosphoramidite group, which is used to obtain a protected single-strand RNA bound to a support.
专利号:US-9963472-B2 优先权日:2013-11-04 标 题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (PKAN) and methods for the synthesis of such compounds 发明人:JENKO BRANKO; KOSEC GREGOR; PETKOVIC HRVOJE; PODGORSEK BERKE AJDA; PAHOR JERCA; CUSAK ALEN; SIBON ODA CORNELIA MARIA; SRINIVASAN BALAJI 权利人:ACIES BIO D O O; UNIV GRONINGEN; ACADEMISCH ZIEKENHUIS GRONINGEN 摘要:The invention relates to (S)-acyl-4′-phosphopantetheine derivatives, methods of their synthesis, and related medical uses of such compounds. Preferred medical uses relate to the treatment of neurodegenerative diseases, such as PKAN.
专利号:US-4255581-A 优先权日:1979-08-13 标题 :Process for the preparation of alkyl and aryl esters of 3'-substituted and 2', 3'-disubstituted 2-anilino-3-pyridinecarboxylic acids 发明人:LOS MARIO A 权利人:LAB BAGO S A 摘要:In this disclosure, the synthesis of alkyl and aryl esters of substituted 2-anilino-3-pyridinecarboxylic acids is described. This preparation is performed reacting a previously obtained alkyl or aryl ester of 2-chloro-3-pyridinecarboxylic acid, with 3,2 or 3-substituted aniline.
专利号:US-9605019-B2 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids 发明人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL 权利人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL; WAVE LIFE SCIENCES LTD 摘要:The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 455. 摘要:Smith, L. H. S.; Coote, S. C.; Procter, D. J., Science of Synthesis Knowledge Updates, (2010) 3, 486.