专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:US-2007065922-A1 优先权日:2005-09-21 标题 :Biocatalytic synthesis of aminodeoxy purine N9-beta-D-nucleosides containing 3-amino-3-deoxy-beta-D-ribofuranose, 3-amino-2,3-dideoxy-beta-D-ribofuranose, and 2-amino-2-deoxy-beta-D-ribofuranose as sugar moieties 发明人:BARAI VLADIMIR N; EROSHEVSKAYA LUDMILLA A; MIKHAILOPULO IGOR A; AZHAYEV ALEX V; LAPINJOKI SEPPO P 权利人:METKINEN OY 摘要:Purine N 9 -β-D-nucleosides containing 3-amino-3-deoxy-β-D-ribofaranose, 3-amino-2,3-dideoxy-β-D-ribofuranose, and 2-amino-2-deoxy-β-D-ribofuranose as sugar moieties are synthesized by biocatalytic transglycosylation of purine bases and the respective 3′-amino-3′-deoxyuridine, 3′-amino-3′-deoxythymidine and 2′-amino-2′-deoxyuridine as donors of the carbohydrate moiety, and the cells of Escherichia coli as a biocatalyst or glutaraldehyde (GA) treated cells of Escherichia coli as a biocatalyst or a mixture of thymidine (uridine) phosphorylase and purine nucleoside phosphorylase.
专利号:US-12060384-B2 优先权日:2019-02-05 标题 :Synthesis of 1,2,5-tri-o-benzoyl-3-dibenzylamino-3-deoxyribose as intermediate for producing 3′-amino-3′-deoxyadenosine and 3′-amino-3′-deoxyguanosine and the protected derivatives thereof 发明人:YUAN CHANGXIA; SCHMIDT MICHAEL ANTHONY; ORTIZ ADRIAN; ROGERS AMANDA J; ZHU JASON J; XU ZHONGMIN; YU MIAO; SIMMONS ERIC M; WU SHULIN 权利人:BRISTOL MYERS SQUIBB CO 摘要:The invention generally relates to improved processes for the preparation of intermediates of a cyclic dinucleotide which is useful as a STING agonist.
专利号:US-3699103-A 优先权日:1970-10-07 标 题 :Process for the manufacture of 5-desoxy-l-arabinose and novel intermediates 发明人:KISS JOSEPH 权利人:HOFFMANN LA ROCHE 摘要:A MULTI-STEP, STEREO-SPECIFIC SYNTHESIS OF 5-DESOXY-LARABINOSE FROM THE READILY AVAILABLE AND INEXPENSIVE STARTING MATERIALS D-GLUCOSE OR D-XYLOSE IS DISCLOSED. 5-DESOXYL-ARABINOSE IS A KNOWN BUILDING BLOCK FOR THE MANUFACTURE OF BIPTERIN, A NATURALLY OCCURING MATERIAL HAVING USES AS A GROWTH FACTOR, AND ANTIOXIDANT, AND AS A PRECURSOR FOR CO-FACTORS OF ENZYMES LEADING TO THE PRODUCTION OF VALUABLE AMINO ACIDS SUCH AS PHENYLALANINE, TRYPTOPHAN AND L-DOPA. L-DOPA IS A VALUABLE MEDICAMENT WHICH HAS RECENTLY BEEN LICENSED IN THIS COUNTRY FOR USE IN THE TREATMENT OF PARKINSON''S DISEASE.
专利号:US-2012289733-A1 优先权日:2011-05-11 标 题 :Novel borate derivatives and their applications 发明人:HEISE GLENN L; MYSLINSKA MALGORZATA 权利人:HEISE GLENN L; MYSLINSKA MALGORZATA; ANDERSON DEV CO 摘要:Borates, compositions comprising chiral (cyclic and acyclic) and achiral (cyclic and acyclic) borates; chiral (cyclic and acyclic) and achiral (cyclic and acyclic) biborates; and methods for their synthesis. Additionally, a significantly improved synthetic protocol for the synthesis of wide range of boronates starting from borates or biborates and Grignard or organolithium reagents that can be used for kilo lab and commercial scale production.
专利号:US-5880294-A 优先权日:1996-05-16 标 题 :D-pentofuranose derivatives and process for preparing the same 发明人:NOMURA MAKOTO; KAZUNO HIDEKI; SATO TSUTOMU; WASHINOSU MASATO; TANAKA MOTOAKI; MATSUDA AKIRA; ASAO TETSUJI 权利人:TAIHO PHARMACEUTICAL CO LTD 摘要:The present invention relates to D-pentofuranose derivatives represented by the following formulas (1) through (4): ##STR1## (wherein A represents a chlorobenzoyl group; R 1 represents a hydrogen atom, an aliphatic lower acyl group, a substituted or unsubstituted benzoyl group; each of X and Y represents a lower alkyl group; Z represents an ethynyl group or tri-lower alkyl silylethynyl group; the sugar moiety in formula (1) represents xylose; and the sugar moiety of each of formulas (3) and (4) represents ribose). The present invention also relates to a process for preparing the compound (2) characterized by oxidizing the compound of formula (1) with a hypochlorite in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidinoxy compound, and these compounds are useful as intermediates in the synthesis of 3'-C-substituted ribonucleoside derivatives having excellent antitumor activities.
摘要:Carbery, D., Science of Synthesis Knowledge Updates, (2010) 3, 159. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Joosten, A.; Brioche, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 6.