专利号:US-6252105-B1 优先权日:1998-07-06 标题:Synthesis of low-fluoride organic compounds 发明人:BRAUN MAX; EICHER JOHANNES; JANSSENS FRANCINE; EICHHOLZ KERSTIN; PALSHERM STEFAN 权利人:SOLVAY FLUOR & DERIVATE 摘要:Organic compounds, e.g. fluorinated organic compounds such as fluorinated carboxylic acids or fluorinated carboxylic acid chlorides, may contain small amounts of carboxylic acid fluorides, hydrogen fluoride or hydrolyzable fluoride, which during the preparation of derivatives of the fluorinated organic compounds, for example by esterification, may yield corrosive fluorides or hydrogen fluoride. The invention is a method for the synthesis and/or purification of preferably fluorinated organic compounds such as carboxylic acids, carboxylic acid chlorides and derivatives such as esters thereof, starting from corresponding carboxylic acid chlorides containing acid fluorides or hydrolyzable fluoride, and alcohols under the catalytic action of 'onium' salts of carboxylic acids, to obtain products which have a low fluoride content. Alternatively, an inorganic oxide adsorbent is utilized. The method is especially suitable for the synthesis of esters of trifluoroacetic acid, chlorodifluoroacetic acid, trifluoroacetoacetic acid and/or difluoroacetoacetic acid.
专利号:US-2024383940-A1 优先权日:2021-03-31 标题 :Synthesis of trinucleotide and tetranucleotide caps for mrna production 发明人:ENDO ATSUSHI 权利人:MODERNA TX INC 摘要:Provided herein are methods of making trinucleotides and tetranucleotides for use as 5′ mRNA caps. The methods utilize a novel “top-downâ€? strategy and provide for synthesis of oligonucleotides with higher yields and increased efficiency compared to traditional methods. A key step of the methods disclosed, herein can also be adapted to utilize a “one-potâ€? approach, resulting in an increase in the yield of the final oligonucleotide product.
专利号:US-2012178710-A1 优先权日:2009-07-01 标题 :Synthesis of cyclic diguanosine monophosphate and thiophosphate analogs thereof 发明人:JONES ROGER A; GAFFNEY BARBARA L 权利人:JONES ROGER A; GAFFNEY BARBARA L; UNIV RUTGERS 摘要:The invention provides methods for the synthesis of cyclic dinucleotides and thiophosphate analogs thereof as well as a new family of analogs of cyclic diguanosine monophosphate that includes a series of seven phosphorothioate derivatives that includes diastereomers of mono-, di-, and trithiophosphates.
专利号:US-7897758-B2 优先权日:2005-04-27 标题 :Activators for oligonucleotide and phosphoramidite synthesis 发明人:WOLTER ANDREAS; LEUCK MICHAEL 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods for the synthesis of oligonucleotides and nucleoside phosphoramidites. The methods are based on employing aryl-substituted 5-phenyl-1H-tetrazoles with perfluoroalkyl groups on the aromatic ring as activators. In one aspect the novel activators are used in the synthesis of oligonucleotides via the phosphoramidite approach. In this aspect the activators are highly efficient and can be applied with very short coupling times. In a further aspect, the activators of the invention are used in the synthesis of phosphoramidites through the reaction of nucleosides comprising a free hydroxyl group with phosphitylating agents. In this aspect the activators provide very pure phosphoramidites under mild conditions. The activators of the invention are further characterized by being highly soluble, non-hygroscopic and non-hazardous.
专利号:US-2023119227-A1 优先权日:2020-02-24 标 题:Oligonucleotide synthesis on solid support 发明人:JI AN; MARVIN MICHAEL; MARKS KEVIN; ANDERSON DAVID 权利人:INTEGRATED DNA TECH INC 摘要:Functionalized solid supports are useful in the synthesis of oligonucleotides. The functionalized solid supports contain an extended linker to a terminal functional group or a first nucleotide or nucleoside moiety. The extended linker permits oligonucleotide synthesis to take place at a greater distance from the solid support with greater efficiency.
专利号:US-8049023-B2 优先权日:2007-12-18 标 题:Reagents and methods for the beta-keto amide synthesis of a synthetic precursor to immunological adjuvant E6020 发明人:DECOSTA BRUCE; FANG FRANCIS G; FOY JAMES E; HAWKINS LYNN; LEMELIN CHARLES; NIU XIANG; WU KUO-MING 权利人:EISAI R&D MAN CO LTD 摘要:This invention relates to the synthesis for a precursor of E6020, compound 26, via a β-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation. n nThe β-keto amide alcohol intermediate compound 22 is a compound of formula (3). Compound 25 is a compound of formula (4).