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:US-2012029226-A1 优先权日:2009-02-06 标题:Method for the synthesis of chiral alpha-aryl propionic acid derivatives 发明人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 权利人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 摘要:The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.
专利号:US-4943630-A 优先权日:1982-10-27 标题 :Method for carrying out the organic synthesis of oligosaccharides containing galactosamine-uronic acid patterns, new oligosaccharides obtained and biological applications thereof 发明人:JACQUINET JEAN-CLAUDE; PETITOU MAURICE; SINAY PIERRE; CHOAY JEAN 权利人:CHOAY SA 摘要:Process for the organic synthesis of oligosaccharides forming or corresponding to fragments of acid mucopolysaccharides wherein two compounds comprised of or terminated respectively by patterns of galactosamine structure and patterns of uronic acid structure. Said patterns are specifically substituted. Said process results in oligosaccharides usable particularly in therapy.
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:EP-0948511-B1 优先权日:1996-12-24 标 题:Chemical synthesis of nucleosides analogs and their incorporation into polynucleotides 发明人:KARPEISKY ALEXANDER; BEIGELMAN LEONID; MATULIC-ADAMIC JASENKA 权利人:SIRNA THERAPEUTICS INC 摘要:Novel nucleosides, process for chemical synthesis of nucleosides and incorporation of the nucleosides into polynucleotides are disclosed. Also described are polynucleotides, such as antisense, TFO and nucleic acid catalysts with one or more modifications, such as 2'-O-amino, L-nucleotides and the others.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
[参考文献]: Takashi Niwa, Et Al. Palladium-Catalyzed 2-Pyridylmethyl Transfer From 2-(2-Pyridyl)Ethanol Derivatives To Organic Halides By Chelation-Assisted Cleavage Of Unstrained C(Sp3 )--C(Sp3) Bonds. Angew Chem Int Ed Engl. 2007;46(15):2643-5.
合成参考文献
摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 409. 摘要:International Labour Office. Encyclopedia of Occupational Health and Safety. Vols. I&II. Geneva, Switzerland: International Labour Office, 1983., p. 1810 摘要:Great Lakes Water Quality Board; Inventory Chem Subst Id Great Lakes Ecos p. 195 (1983) 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要:M. Tissier and C. Tissier. Bull. Soc. Chim. France 1967, 3155.