专利号:US-8268936-B2 优先权日:2005-01-04 标题:Synthesis of hybrid block copolymers and uses thereof 发明人:BREITENKAMP KURT; SILL KEVIN N 权利人:BREITENKAMP KURT; SILL KEVIN N; INTEZYNE TECHNOLOGIES INC 摘要:The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and methods of preparing the same.
专利号:US-2009177008-A1 优先权日:2005-12-28 标题:Novel process for synthesis of itopride and its novel intermediate n-(4-hydroxybenzyl)- 3,4-dimethoxybenzamide 发明人:KHAMAR BAKULESH MAFATLAL; MODI INDRAVADAN AMBALAL; VENKATRAMAN JAYARAMAN; RAVI PONNAIAH; NORI DIVAKARA SOMAYAJULU; GAJULA MADHUSUDANA RAO; RENUGADEVI GURUSAMY; SHASHIKALA KUNJARU N; RUDRAMUNI SANTOSH M 权利人:CADILA PHARMACEUTICALS LTD 摘要:The present invention relates to a novel and improved process for the preparation of N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide—known as Itopride, via a novel intermediate N-(4Ëœhydroxybenzyl)-3,4-dimethoxybenzamide.
专利号:US-8895741-B2 优先权日:2003-06-03 标 题:Process for the synthesis of biaryl oxazolidinones 发明人:WU YUSHENG; CHEN SHILI; CHEN YI; HANSELMANN ROGER; LOU RONGLIANG; ZHOU JIACHENG 权利人:WU YUSHENG; CHEN SHILI; CHEN YI; HANSELMANN ROGER; LOU RONGLIANG; ZHOU JIACHENG; MELINTA THERAPEUTICS INC 摘要:The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
专利号:US-12024483-B2 优先权日:2019-11-13 标题 :Synthesis method of hydroxybenzylamine 发明人:XU CHANGPING; JIA YANRONG 权利人:TAIZHOU CHUANGYUAN INDUSTRIAL TECH CO LTD 摘要:The present invention relates to a synthesis method of hydroxybenzylamine, belonging to the technical field of organic synthesis. The principle of the method is a demethylation reaction of methoxybenzylamine in the presence of hydrobromic acid. The present invention has the characteristics that methoxybenzylamine and hydrobromic acid are distilled at reflux to remove redundant water to improve a reaction temperature and increase the concentration of hydrobromic acid in a reaction mixture, thereby enhancing the demethylation of hydrobromic acid on methoxybenzylamine and then shortening a reaction time and increasing a conversion rate; when generation of a methyl bromide gas is not observed, distillation is continued, excess hydrobromic acid is recycled to further improve the reaction temperature and increase the conversion rate and meanwhile reduce the consumption of raw material hydrobromic acid and decrease the processing capacity of the subsequent steps and the consumption of raw material sodium hydroxide.
专利号:US-8431693-B2 优先权日:2004-04-05 标题:Process for desilylation of oligonucleotides 发明人:MANOHARAN MUTHIAH; JUNG MICHAEL F; RAJEEV KALLANTHOTTATHIL G; PANDEY RAJENDRA K; WANG GANG 权利人:MANOHARAN MUTHIAH; JUNG MICHAEL F; RAJEEV KALLANTHOTTATHIL G; PANDEY RAJENDRA K; WANG GANG; ALNYLAM PHARMACEUTICALS INC 摘要:The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups. In a preferred embodiment, the acrylonitrile scavenger is a polymer-bound thiol. Another aspect of the present invention relates to agents used to oxidize a phosphite to a phosphate. In a preferred embodiment, the oxidizing agent is sodium chlorite, chloroamine, or pyridine-N-oxide. Another aspect of the present invention relates to methods of purifying an oligonucleotide by annealing a first single-stranded oligonucleotide and second single-stranded oligonucleotide to form a double-stranded oligonucleotide; and subjecting the double-stranded oligonucleotide to chromatographic purification. In a preferred embodiment, the chromatographic purification is high-performance liquid chromatography.
专利号:WO-2011028218-A1 优先权日:2009-09-02 标 题 :Process for triphosphate oligonucleotide synthesis 发明人:ZLATEV IVAN; MORVAN FRANCOIS; VASSEUR JEAN-JACQUES; DEBART FRANCOISE; MANOHARAN MUTHIAH 权利人:ALNYLAM PHARMACEUTICALS INC; CENTRE NAT RECH SCIENT; ZLATEV IVAN; MORVAN FRANCOIS; VASSEUR JEAN-JACQUES; DEBART FRANCOISE; MANOHARAN MUTHIAH 摘要:The present invention describes simple, efficient, and enzyme-free method of making oligonucleotides with 5'-triphosphate. This invention presents novel process for synthesizing triphosphate oligonucleotides using a diaryl phosphonate as reagent. The process of the present invention is amenable to large-scale, economic 5 '-triphosphate oligonucleotide synthesis.
Kirabo, A., Fontana, V., de Faria, A.P.C., et al. DC isoketal-modified proteins activate T cells and promote hypertension J. Clin. Invest. 124(10), 4642-4656 (2014).
合成参考文献
摘要:Bagal, D. B.; Bhanage, B. M., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2018) 2, 396. 摘要:J. Epstein, R. E. Plapinger, H. O. Michel, J. R. Cable, R. A. Stephani, R. J. Hester, C. Billington and G. R. List, J. Am. Chem. Soc. 86, 3075 (1964). 摘要:Sharma, U.; Parmar, D.; Sumit; Manisha, Science of Synthesis: Knowledge Updates, (2024) 2, 16.