专利号:US-6998484-B2 优先权日:2000-10-04 标 题:Synthesis of purine locked nucleic acid analogues 发明人:KOCH TROELS; JENSEN FLEMMING REISSIG 权利人:SANTARIS PHARMA AS 摘要:The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.
专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-2003170698-A1 优先权日:2002-01-04 标题 :Droplet-based microfluidic oligonucleotide synthesis engine 发明人:GASCOYNE PETER; VYKOUKAL JODY V; SCHWARTZ JON; BECKER FREDERICK F 摘要:Devices, systems, and methods for an oligonucleotide synthesis engine. In on embodiment, the invention involves a microfluidic device including: an oligonucleotide synthesis subunit including a reaction surface and means for generating a manipulation force and routing for packet delivery; an analysis or diagnostic subunit; and a control subunit including a program to direct oligonucleotide synthesis. In another embodiment, the invention involves a method for analyzing a sample. An oligonucleotide is synthesized in a solid-phase oligonucleotide synthesis subunit, wherein the subunit includes a reaction surface and means for generating a manipulation force and routing for packet delivery. The synthesis is controlled with a control subunit, wherein the control subunit is programmed for the automatic synthesis of oligonucleotides. The sample is analyzed in an analysis or diagnostic subunit.
专利号:US-8729310-B2 优先权日:2009-09-22 标题:Halogenated diarylamine compound and synthesis method thereof 发明人:OSAKA HARUE; INOUE HIROTO 权利人:OSAKA HARUE; INOUE HIROTO; SEMICONDUCTOR ENERGY LAB 摘要:An object is to provide a new halogenated diarylamine compound serving as a source material for synthesis of a variety of diarylamine compounds and triarylamine compounds and a synthesis method of the new halogenated diarylamine compound. A halogenated diarylamine compound represented by the following general formula (G1) and a synthesis method thereof are provided. Note that a variety of diarylamine compounds and triarylamine compounds can be synthesized using the halogenated diarylamine compound represented by the following general formula (G1).
专利号:US-7202362-B2 优先权日:2003-03-07 标 题 :Transition metal complexes from solid state synthesis 发明人:THUMMEL RANDOLPH P; HU YI-ZHEN 权利人:UNIV HOUSTON 摘要:Methods and compositions related to the synthesis of photosensitizers of titanium dioxide performed in situ, stepwise, in the solid state, and directly on the surface of the titanium dioxide semiconductor material. The method is generally accomplished by first absorbing an anchor ligand onto the titanium dioxide semiconductor material, then adding an appropriate transition metal, and finally adding one or more secondary ligands to complete the synthesis of the transition metal complex or sensitizer.
摘要:Zysman-Colman, E., Science of Synthesis, (2010) 45, 175. 摘要:Zysman-Colman, E., Science of Synthesis, (2010) 45, 182. 摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 47, 460. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 638. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 193.