专利号:WO-2023233371-A1 优先权日:2022-06-03 标 题:A continuous flow process for synthesis of organic azides 发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE 摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.
专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
专利号:US-9862733-B2 优先权日:2010-07-23 标题 :Apparatus and methods for the automated synthesis of small molecules 发明人:BURKE MARTIN D; GILLIS ERIC P; BALLMER STEVEN G 权利人:BURKE MARTIN D; GILLIS ERIC P; BALLMER STEVEN G; UNIV ILLINOIS 摘要:Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention. Coupling and other reactions embraced by the invention include, without limitation, Suzuki-Miyaura coupling, oxidation, Swern oxidation, “Jones reagentsâ€? oxidation, reduction, Evans' aldol reaction, HWE olefination, Takai olefination, alcohol silylation, desilylation, p-methoxybenzylation, iodination, Negishi cross-coupling, Heck coupling, Miyaura borylation, Stille coupling, and Sonogashira copling.
专利号:US-12344881-B2 优先权日:2023-09-27 标题 :Genetic engineering bacterium for de novo synthesis of cis,cis-muconic acid by taking glucose as substrate and applications thereof 发明人:TAN TIANWEI; LI MENGLEI 权利人:UNIV BEIJING CHEM TECH 摘要:The present invention discloses a genetic engineering bacterium for de novo synthesis of cis,cis-muconic acid by taking glucose as a substrate and applications thereof, and belongs to the technical field of genetic recombination and metabolic engineering. The genetic engineering bacterium for de novo synthesis of cis,cis-muconic acid (MA) by taking glucose as the substrate disclosed in the present invention is modified with chassis microbes, and includes recombinant Corynebacterium glutamicum for a cis,cis-muconic acid pathway construction module and an intermediate high-yield module. Production capacity of strains is greatly improved; MA of 90.2 g/L is finally obtained in fermentation liquor; and possibilities are provided for green and low-cost production of numerous chemicals such as adipic acid and nylon-66.
专利号:US-8278483-B2 优先权日:2006-02-07 标题:Process for synthesis of glycomimicking cationic amphiphiles 发明人:MAHIDHAR YENUGONDA VENKATA; CHAUDHURI ARABINDA; MUKHERJEE RAMA 权利人:MAHIDHAR YENUGONDA VENKATA; CHAUDHURI ARABINDA; MUKHERJEE RAMA; COUNCIL SCIENT IND RES 摘要:The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.
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.
1: Josyula JVN, JeanPierre AR, Jorvekar SB, Adla D, Mariappan V, Pulimamidi SS, Green SR, Pillai AB, Borkar RM, Mutheneni SR. Metabolomic profiling of dengue infection: unraveling molecular signatures by LC-MS/MS and machine learning models. Metabolomics. 2024 Sep 21;20(5):104. doi: 10.1007/s11306-024-02169-0. 229:116524. doi: 10.1016/j.bcp.2024.116524. Epub ahead of print. 412:131403. doi: 10.1016/j.biortech.2024.131403. Epub 2024 Aug 31. 13(9):2873-2886. doi: 10.1021/acssynbio.4c00287. Epub 2024 Aug 29. 279(Pt 1):135099. doi: 10.1016/j.ijbiomac.2024.135099. Epub ahead of print.
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