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-5719283-A 优先权日:1990-06-20 标 题:Intermediates useful in the synthesis of pyrazolopyrimidinone antianginal agents 发明人:BELL ANDREW SIMON; BROWN DAVID; TERRETT NICHOLAS KENNETH 权利人:PFIZER 摘要:Compounds of the formula ##STR1## wherein R 1 is H, C 1 -C 3 alkyl, C 3 -C 5 cycloalkyl or C 1 -C 3 perfluoroalkyl; n R 2 is H, C 1 -C 6 alkyl optionally substituted by OH, C 1 -C 3 alkoxy or C 3 -C 6 cycloalkyl, or C 1 -C 3 perfluoroalkyl; n R 3 is H, C 1 -C 6 alkyl, C 3 -C 6 alkenyl, C 3 -C 6 alkynyl, C 3 -C 7 cycloalkyl, C 1 -C 6 perfluoroalkyl or (C 3 -C 6 cycloalkyl)C 1 -C 6 alkyl; n and Y is chloro, bromo, or fluoro. n The above compounds are intermediates useful in the synthesis of certain pyrazolopyrimidinones which inhibit cyclic guanosine 3', 5'-monophosphate phosphodiesterase.
专利号:WO-2016147205-A1 优先权日:2015-03-13 标题 :Novel substituted 3-spirophosphoryl pyrazole-2-oxindoles as anti-infectives and process for the synthesis thereof 发明人:SURYAVANSHI GURUNATH MALLAPPA; SHELKE ANIL MARUTI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to novel substituted 3-spirophosphoryl, pyrazole-2-oxindoles of Formula (I) and its pharmaceutically acceptable salts, esters, ethers, isomers, stereoisomers, positional isomers and pplymorphs. The present invention further relates to one pot, one step process for the synthesis of spirophosphoiyl pyrazole oxindoles of Formula (I) with yield in the range of 70-85%.
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.