专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
专利号:US-5286901-A 优先权日:1990-03-09 标题:Prescursors for and synthesis of mono- and difunctionalized acetylenes and difunctional 1,3-diynes 发明人:STANG PETER J; CRITTELL CHARLES M; WILLIAMSON BOBBY L; ZHDANKIN VIKTOR 权利人:UNIV UTAH RES FOUND 摘要:Precursors and methods for the synthesis of mono- and difunctionalized acetylenes are described. The invention includes novel tricoordinate iodonium transfer reagents and novel alkynyldi(phenyliodonium) salts, both of which are precursors for the functionalized acetylenes. The iodonium transfer reagents take the general form of mixed iodonium sulfonates PhI + (X)OSO 2 R f , where X may be OAc, NHAc, NCO, or CN. These mixed iodonium sulfonates are produced by reaction of iodosobenzene with certain substituted trimethylsilanes. n To make the alkynyldi(phenyliodonium) salt PhI + C.tbd.CI + Ph•2 R f SO 3 - ,a mixed iodonium sulfonate is reacted with a bistin acetylene of the kind R' 3 SnC.tbd.CSnR' 3 . Alternatively, the reaction may be performed with disubstituted tin diacetylenes to produce PhI + C.tbd.C-C.tbd.CI + Ph•2 R f SO 3 - to produce a dialkynyldi(phenyliodonium) salt. Subsequent reaction of a nucleophile with the alkynyldi(phenyl-iodonium) salt or dialkynyldi(phenyliodonium) salt produces a difunctional acetylene or a difunctional 1,3-diyne, respectively.
专利号:US-8183355-B2 优先权日:2006-04-28 标题 :Method for the synthesis of oligonucleotide derivatives 发明人:MORVAN FRANCOIS; MEYER ALBERT; VASSEUR JEAN-JACQUES; VIDAL SEBASTIEN; CLOAREC JEAN-PIERRE; CHEVOLOT YANN; SOUTEYRAND ELIANE 权利人:MORVAN FRANCOIS; MEYER ALBERT; VASSEUR JEAN-JACQUES; VIDAL SEBASTIEN; CLOAREC JEAN-PIERRE; CHEVOLOT YANN; SOUTEYRAND ELIANE; CENTRE NAT RECH SCIENT 摘要:Method for the synthesis of nucleotide derivatives wherein molecules of interest are grafted on the oligonucleotide with the help of a “click chemistryâ€? reaction between an azide function on the molecule of interest and an alkyne function on the oligonucleotide, or between an alkyne function on the molecule of interest and an azide function on the oligonucleotide. n Intermediate molecules, notably alkyne functionalized oligonucleotides, grafted oligonucleotides, azide functionalized oligonucleotides, oligonucleotide micro arrays containing them and the use of those grafted oligonucleotides for biological investigation and for cell targeting.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:WO-2025083208-A1 优先权日:2023-10-19 标题 :Synthesis of morpholine derivatives and compounds therefore 发明人:BUESCHLEB MARTIN; BEAUFILS FLORENT; PROUDFOOT JOHN 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a synthesis method for morpholine derivatives, including a ring-formation out of a 1,2-amino alcohol and a compound of formula (I) whereby LG is a nucleophilic leaving group and R1 to R7 are as herein defined.
专利号:US-10815178-B2 优先权日:2015-12-21 标 题:Intermolecular reaction of propargyl ethers with dimethylfuran in the presence of gold(I) complexes 发明人:LETINOIS ULLA; ACKERMANN STEPHAN; MEDLOCK JONATHAN ALAN; LEHMANN HAJO 权利人:DSM IP ASSETS BV 摘要:The present invention relates to a method of preparing ortho substituted phenols from 2,5-dimethylfuran and propargyl ethers in the presence of a gold(I) complex. It is particularly advantageous to use 2,5-dimethylfuran as this offers an ecological beneficial synthesis of said ortho substituted phenols.
摘要:Baird, M. S., Science of Synthesis, (2010) 47, 1111. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 25. 摘要:Aguilar, E.; López, L. A., Science of Synthesis Knowledge Updates, (2014) 2, 116. 摘要:Durand, A.; Hemeon, I.; Singer, R. D., Science of Synthesis Knowledge Updates, (2013) 2, 144. 摘要:Sainsbury, M., Science of Synthesis Knowledge Updates, (2010) 1, 239.