专利号:US-6809195-B1 优先权日:2000-08-16 标 题:Process for the preparation of oligonucleotides 发明人:SANGHVI YOGESH S; SONG QUANLAI 权利人:ISIS PHARMACEUTICALS INC 摘要:The present invention discloses methods for synthesizing oligomeric compounds. The methods include a modified phosphoramidite protocol wherein the oxidation and capping steps are combined into a single step. The methods result in increased efficiency and are especially amenable to the large scale synthesis of oligomeric compounds.
专利号:US-7579459-B2 优先权日:2005-12-12 标 题 :Activator bound solid supports for nucleic acid synthesis via the phosphoramidite approach 发明人:NGO NAM Q; JAQUINOD LAURENT 权利人:NGO NAM Q; JAQUINOD LAURENT 摘要:The present invention relates to improved methods for the preparation of nucleic acids. More particularly, conventional solid supports used for nucleic acid synthesis are derivatized with activators having pKas within the 4 to 7 range. Preferentially, CPG-based solid supports are reacted with trialkoxysilanes containing an activator moiety such as pyridine. During each deblocking step of the nucleic acid synthesis cycle, bound pyridiniums are generated, yielding a weak acidic medium spreads throughout the solid support. The bound activators efficiently activate the phosphoramidite reagents towards coupling with 5′-hydroxynucleosides bound to the solid supports, thus eliminating or supplementing external deliveries of activator during the coupling steps.
专利号:RU-2141321-C1 优先权日:1994-03-04 标题:Use of imidazole derivatives for preparing pharmaceutical composition showing activity to angiotensin receptors at1 and at2, some of these compounds, method of synthesis of imidazole derivatives and pharmaceutical composition based on thereof
专利号:US-6762281-B2 优先权日:2000-09-08 标题:Process for preparing peptide derivatized oligomeric compounds 发明人:MANOHARAN MUTHIAH; GUZAEV ANDREI P 权利人:ISIS PHARMACEUTICALS INC 摘要:Methods of preparing peptide linked oligomeric compounds are provided. The method is useful for preparing larger scale amounts of peptide linked oligomeric compounds. More particularly, the synthesis of peptide linked oligomeric compounds is performed without the problems of aggregation associated with electrostatic interactions. The present method describes using equimolar amounts of oligomeric compounds and peptide reagents providing for an increase in overall efficiency.
专利号:RU-2174513-C2 优先权日:1994-03-04 标 题 :Tetrasubstituted derivatives of imidazole, methods of their synthesis, intermediate compounds and pharmaceutical composition
[参考文献]: M Muneer, Et Al. Semiconductor-Mediated Photocatalysed Degradation Of Two Selected Pesticide Derivatives, Terbacil And 2,4,5-Tribromoimidazole, In Aqueous Suspension. Water Sci Technol. 2001;44(5):331-7. [参考文献]: R D Verschoyle, Et Al. The Relationship Between Uncoupling Of Oxidative Phosphorylation And Neuronal Necrosis Within The Cns In Rats Dosed With Trihalogenated Imidazoles. Toxicol Appl Pharmacol. 1987 Jun 30;89(2):175-82. [参考文献]: R D Verschoyle, Et Al. The Toxicity And Neuropathology Of 2,4,5-Tribromoimidazole And Its Derivatives In Rats. Arch Toxicol. 1984 Dec;56(2):109-12. [参考文献]: Tun-Cheng Chien, Et Al. Synthesis And Antiviral Evaluation Of Polyhalogenated Imidazole Nucleosides: Dimensional Analogues Of 2,5,6-Trichloro-1-(Beta-D-Ribofuranosyl)Benzimidazole. J Med Chem. 2004 Nov 4;47(23):5743-52.
合成参考文献
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#05092 摘要:Archives of Toxicology., 56(109), 1984 [] 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).