专利号:US-7807821-B1 优先权日:2004-03-01 标题 :Method for the synthesis of nucleic acid without protecting base moiety 发明人:SEKINE MITSUO; SEIO KOHJI; OHKUBO AKIHIRO 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:A phosphoramidite method for the synthesis of a nucleic acid oligomer without protecting the base moiety characterized in that a 3′ or 5′ hydroxyl group of a nucleotide is reacted with a nucleoside phosphoramidite, a cyclonucleoside phosphoramidite, a 2′-substituted nucleoside phosphoramidite, a 4′-substituted nucleoside phosphoramidite, or a 2′,4′-di-substituted nucleoside phosphoramidite to produce a phosphodiester linkage. The phosphoramidite is contacted with an activator containing both a) hydroxybenzotriazole-1-ol (HOBt), a mono-substituted HOBt, a di-substituted HOBt, or a di-substituted phenol and b) imidazole, tetrazole, benzimidazoletriflate (BIT), 4-ethylthiotetrazole, imidazolium triflate(trifluoromethane sulfonate) or 4,5-dicyanoimidazole.
专利号:US-2014309424-A1 优先权日:2011-06-30 标题:Direct synthesis of 18f-fluoromethoxy compounds for pet imaging and the provision of new precursors for direct radiosynthesis of protected derivatives of o-([18f] fluoromethyl) tyrosine 发明人:BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN 权利人:BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN; PIRAMAL IMAGING SA 摘要:The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18 F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([ 18 F]Fluoromethyl)tyrosines.
专利号:US-6310198-B1 优先权日:1993-01-08 标题:Extremely high purity oligonucleotides and methods of synthesizing them using dimer blocks 发明人:TANG JIN-YAN; BONGLE NANDKUMAR; GONZALEZ JOSE; SCHWARTZ WARREN E 权利人:AVECIA BIOTECHNOLOGY INC 摘要:The present invention comprises an improved method of synthesizing oligonucleotides. The method comprises employing dinucleotides (or 'dimer blocks') as the basic synthetic unit building block. The method results in extremely high purity oligonucleotides in which the N-1 content is very low, generally less than 1-2% of the full length, N, oligonucleotide. We have found that synthesis using dinucleotide phosphorothioates results in oligonucleotides having very little phosphodiester content. Furthermore, we have found that the amount of dimer required in each coupling step can be less than about 6 and is preferably about 2 equivalents. Synthesis of oligonucleotides according to the dimer block approach described herein can also be conducted without the capping step that has heretofore been deemed necessary after each coupling.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-3725380-A 优先权日:1969-04-05 标 题:Method of synthesizing peptides in the presence of a carbodiimide and a 1-hydroxy-benzotriazole 发明人:KONIG W; GEIGER R 权利人:HOECHST AG 摘要:Improved synthesis of peptides by the carbodiimide method in which an amino-protected amino acid or peptide having a reactive carboxy group is condensed with a carboxy-protected amino acid or peptide having a reactive amino group in the presence of a 1hydroxy-benzotriazole or a substituted 1-hydroxy-benzotriazole of the formula AS WELL AS IN THE PRESENCE OF A CARBODIIMIDE SUCH AS DICYCLOHEXYL CARBODIIMIDE.
专利号:KR-20140063577-A 优先权日:2011-06-30 标 题 :Direct synthesis of 18F-fluoromethoxy compounds for PET imaging and the provision of novel precursors for direct radiative synthesis of protected derivatives of O - ([18F] fluoromethyl) tyrosine