苯甲醛吖嗪置于phosphate Buffer体系中,用 甲醇,水 用作溶剂,化学反应生成苄胺 参考文献:Goyal,R. N.; Minocha,Ashwani; Singh,U. R.,Indian Journal Of Chemistry,Section A: Inorganic,Physical,Theoretical And Analytical,1985,Vol. 24,# 8,P. 661-664 标题:Goyal,R. N.; Minocha,Ashwani; Singh,U. R.,Indian Journal Of Chemistry,Section A: Inorganic,Physical,Theoretical And Analytical,1985,Vol. 24,# 8,P. 661-664
专利信息
专利号:US-11566040-B2 优先权日:2019-01-28 标题:Synthesis of O-antigen oligosaccharide compounds of Helicobacter pylori serotype O2 发明人:YIN JIAN; HU JING; LIU ZHONGHUA; QIN CHUNJUN 权利人:UNIV JIANGNAN 摘要:Disclosed is synthesis of an O-Antigen oligosaccharide compound of Helicobacter pylori serotype O2, belonging to the field of organic synthesis. The disclosure obtains O-antigen disaccharide to tetracosasaccharide of Helicobacter pylori serotype O 2 by chemical synthesis. A chemical synthesis method which is quite conducive to production of a glucose-α-lglucosidic bond is developed in the disclosure by a protectant strategy, temperature effect, solvent effect, and additive effect. The method is applied in synthesis of an O-antigen oligosaccharide compound of Helicobacter pylori serotype O2 assembled with an amino linking arm. A saccharide conjugate can be prepared from the synthesized O-antigen oligosaccharide compound of Helicobacter pylori serotype O2 assembled with an amino linking arm together with a carrier protein for immunology researches, playing an important role in preventing and treating Helicobacter pylori.
专利号:US-5977301-A 优先权日:1992-09-24 标题 :Synthesis of N-substituted oligomers 发明人:ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:US-7479569-B2 优先权日:2004-02-13 标题:Process for the synthesis of (7-methoxy-3,4-dihydro-1-naphthalenyl) acetonitrile and its application in the synthesis of agomelatine 发明人:SOUVIE JEAN-CLAUDE; GONZALEZ BLANCO ISAAC 权利人:SERVIER LAB 摘要:A process for the industrial synthesis of the compound of formula (I) n nApplication in the synthesis of agomelatine.
专利号:EP-0671928-B1 优先权日:1992-09-24 标题 :Synthesis of n-substituted oligomers 发明人:ZUCKERMANN RONALD N; KERR JANICE M; KENT STEPHEN BRIAN HENRY; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R<9>) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using the automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-8853220-B1 优先权日:2011-02-25 标题 :Synthesis of 2,6,9-tri-substituted-4,8-dinitro-2,6,9-triazabicyclo[3.3.1]nona-3,7-diene intermediates toward the preparation of polyaza-adamantanes 发明人:STERN ALFRED G; DIAMOND CRAIG J 权利人:STERN ALFRED G; DIAMOND CRAIG J; US NAVY 摘要:The present invention relates to methods for synthesizing energetic compounds and intermediates thereof. Specifically, the present invention relates to methods for synthesizing adamantanes and intermediates that are useful in such synthesis. Synthesized intermediates are useful in the synthesis of bicyclic and tricyclic substituted adamantanes. Examples of various intermediates are: acyclic 2-nitromalonaldehyde intermediates, 2,6,9-tri-substituted-4,8-dinitro-2,6,9-triazabicyclo[3.3.1]nona-3,7-dienes and 2,6-dinitro-4,8,9,10-tetra-aza-4,8,9,10-tetra-substituted adamantanes. Intermediates synthesized according to the methods of the present invention are useful toward the synthesis of tetraaza-adamantanes, which can serve as precursors to potentially superior new high-energy-density compounds (HEDCs). The tricyclic intermediate compound has a structure of Formula III: n n n n n n n n n n n n where R is one of a benzyl, 4-methoxybenzyl, acetyl, nitro, formyl, allyl, and a carboethoxyl group.
参考文献:10.1021/bi901933d 摘要:Chang CM, Klema VJ, Johnson BJ, Mure M, Klinman JP, Wilmot CM. Kinetic and structural analysis of substrate specificity in two copper amine oxidases from Hansenula polymorpha. Biochemistry. 2010 Mar 23;49(11):2540–50. 参考文献:10.1002/cmdc.201100262 摘要:Guillon R, Pagniez F, Rambaud C, Picot C, Duflos M, Logé C, Le Pape P. Design, synthesis, and biological evaluation of 1-[(biarylmethyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as potent antifungal agents: new insights into structure-activity relationships. ChemMedChem. 2011 Oct 04;6(10):1806–15. doi: 10.1002/cmdc.201100262. 参考文献:10.1007/s11010-011-0953-8 摘要:Makowska M, Łukowska-Chojnacka E, Wińska P, Kuś A, Bilińska-Chomik A, Bretner M. Design and synthesis of CK2 inhibitors. Molecular and Cellular Biochemistry. 2011 Jul 13;356(1-2):91. doi: 10.1007/s11010-011-0953-8. 参考文献:10.1107/s1600536811006258 摘要:Ponugoti PR, Penthala NR, Dwoskin LP, Parkin S, Crooks PA. cis-1-Benzyl-pyrrolidine-2,5-dicarbonitrile. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o747. 参考文献:10.1107/s1600536811013183 摘要:Li Z, Nie W, Borzov MV. rac-(OC-6-33)-bis[2-(N-Benzylmethyliminomethyl-κN)-1H-imidazol-1-ido-κN1]bis(ethylamido)titanium(IV). Acta Crystallogr E Struct Rep Online. 2011 Apr 13;67(5):m590–1. doi: 10.1107/s1600536811013183.