4-碘吡唑置于硝酸体系中,用 四氢呋喃 用作溶剂,化学反应 2.5H,以92%的收率获得4-硝基吡唑 参考文献:Silica-sulfuric Acid Catalyzed Nitrodeiodination Of Iodopyrazoles 标题:Silica-sulfuric Acid Catalyzed Nitrodeiodination Of Iodopyrazoles 摘要:We Report Here The Synthesis Of Nitropyrazoles In Good To Excellent Yields From Iodopyrazoles Over Silica-Sulfuric Acid Catalyst For The First Time. The Present Procedure Require Less Acid,Offers A Simplified Workup Procedure,And May Be Applied For The Nitration Of A Wide Variety Of Iodoazoles In Drug And Pharmaceutical Industries. Doi:10.1080/00397911.2011.584261
专利号:US-11319291-B1 优先权日:2020-06-09 标 题:Continuous flow microfluidic process for synthesis of 3,4-dinitropyrazole 发明人:SCHROER THORSTEN G; LECROY GREGORY E; RODRIGUEZ MAYRA P; WANG SIDA; AGUILA MIGUEL 权利人:US GOV AIR FORCE; US AIR FORCE 摘要:Disclosed herein is a synthetic method, apparatus, and system for the continuous-flow synthesis of 3,4-dinitropyrazole from pyrazole in a microfluidic environment. This synthetic strategy consist of three (3) synthetic steps, including (1) N-nitration of pyrazole, (2) thermal rearrangement into 3-nitropyrazole, and (3) 4-nitration of 3-nitropyrazole. The current technique produces 3,4-dinitropyrazole in yields up to 85% in particular embodiments, in comparison to 40-50% yields demonstrated by the current state of-the-art batch process for large scale synthesis from pyrazole.
专利号:US-2023212204-A1 优先权日:2020-01-16 标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds 发明人:XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI 权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST 摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.
专利号:US-9936723-B2 优先权日:2014-02-12 标题 :Process for the synthesis of substituted 1-benzyl-3-(1-(isoxazol-4-ylmethyl)-1h-pyrazol-4-yl)imidazolidine-2,4-diones 发明人:FOTSING JOSEPH R 权利人:SENOMYX INC 摘要:The present invention relates to processes and intermediates for the preparation of compounds of formula (I): n nor a salt or oxide thereof, wherein Alk, M1, M2, R1, R2, R3, R4, R5, R6, R7, and n are as described herein. The present invention also relates to compounds of formula (I) and composition comprising a compound of formula (I). Also disclosed is a method of altering or improving the taste of a composition that includes adding to the composition at least one compound of formula (I), in an amount effective to obtain a modified composition having altered or improved taste relative to an otherwise identical composition lacking said compound.
专利号:US-11696954-B2 优先权日:2017-04-28 标题 :Synthesis of spherical nucleic acids using lipophilic moieties 发明人:KANG RICHARD; NALLAGATLA SUBBARAO; ANDERSON BART; KANDIMALLA EKAMBAR 权利人:EXICURE OPERATING COMPANY 摘要:Spherical nucleic acids (SNA) carrying self-aggregating oligonucleotides are described herein. Compositions of the SNA include discrete nanostructures that are not aggregated. Related methods are also described.
专利号:US-5663366-A 优先权日:1992-10-16 标 题:Process for the synthesis of 4,5-diaminopyrazole derivatives useful for dyeing hair 发明人:NEUNHOEFFER HANS; GERSTUNG STEFAN; CLAUSEN THOMAS; BALZER WOLFGANG R 权利人:WELLA AKTIENGESELLSCHAT 摘要:The subject matter of the present invention is directed to a process for producing 4,5-diaminopyrazole derivatives of the general formula (I) (I) where R1 and R2 independently designate hydrogen, a C1- to C6-alkyl radical or a C2- to C4-hydroxyalkyl radical, which can be used as dye precursors, for example for hair dyes, and to new pyrazole derivatives. When using the process according to the invention good yields of isomer-pure 4,5-diaminopyrazole derivatives of general formula (I) can be obtained.
专利号:US-12018251-B2 优先权日:2017-10-13 标 题:Method for synthesis of polynucleotides using a diverse library of oligonucleotides 发明人:VLADAR HAROLD PAUL; FERNANDES REDONDO RODRIGO APARECIDO 权利人:RIBBON BIOLABS GMBH 摘要:A method for synthesizing a target double stranded (ds) polynucleotide byproviding an oligonucleotide library within an array device that has a diversity of oligonucleotide library members, each of which has a different nucleotide sequence and is contained in a separate library containment in an aqueous solution. The library includes single stranded oligonucleotides and double stranded oligonucleotides with at least one overhang and covers at least 10,000 pairs of matching oligonucleotides. In a first step, at least a first pair of matching oligonucleotides are transferred transferred from the library into a first reaction containment using a liquid handler and the matching oligonucleotides are assembled, thereby obtaining a first reaction product comprising at least one overhang. Further reaction products are then likewise obtained and are assembled in a predetermined workflow using an algorithm, thereby producing said target ds polynucleotide with an overhang, optionally followed by a finalization step to prepare blunt ends.
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 171. 摘要:Campagne, J. M.; Leclerc, E., Science of Synthesis Knowledge Updates, (2020) 2, 178. 摘要:Galczynski, J.; Huang, H.; Lambert, T. H., Science of Synthesis: Special Topics, (2021) 1, 329. 摘要:J. Elguero, E. Gonzalez and R. Jacquier. Bull. Soc. Chim. France 1968, 5009. 参考文献:10.1002/chem.200800329 摘要:Seeliger F, Błażej S, Bernhardt S, Mąkosza M, Mayr H. Reactions of Nitroheteroarenes with Carbanions: Bridging Aromatic, Heteroaromatic, and Vinylic Electrophilicity. Chemistry A European J. 2008 Jul 04;14(20):6108–18. doi: 10.1002/chem.200800329.