6-Cyano-9-(Tetrahydropyran-2-yl)Purine置于dowex 50X8 (H+),水体系中,用 甲醇 用作溶剂,化学反应 1.0H,以95%的收率获得6-氰嘌呤 参考文献:A Facile Synthesis Of 6-Cyanopurine Bases 标题:A Facile Synthesis Of 6-Cyanopurine Bases 摘要:报道了一种从市售6-氯嘌呤制备6-氰基嘌呤碱的简便方法.将6-氯嘌呤选择性地保护为thp基团,保护衍生物与四乙基铵氰和dabco反应,得到6-氰基嘌呤衍生物,易于脱保护得到目标化合物. Doi:10.1135/cccc19951386
专利号:US-11453697-B1 优先权日:2015-08-13 标题 :Cyclic di-nucleotide compounds as sting agonists 发明人:ALTMAN MICHAEL D; ANDRESEN BRIAN; CHANG WONSUK; CUMMING JARED N; OTTE RYAN D; TROTTER BENJAMIN WESLEY 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base 1 , Base 2 , Y, Y a , X a , X a1 , X b , X b1 , X c , X c1 , X d , X d1 , R 1 , R 1a , R 2 , R 2a , R 3 , R 4 , R 4a , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , and R 8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
专利号:US-8440810-B2 优先权日:2002-09-20 标 题:Riboswitches, methods for their use, and compositions for use with riboswitches 发明人:BREAKER RONALD R; NAHVI ALI; SUDARSAN NARASIMHAN; EBERT MARGARET S; WINKLER WADE; BARRICK JEFFREY E; WICKISER JOHN K 权利人:BREAKER RONALD R; NAHVI ALI; SUDARSAN NARASIMHAN; EBERT MARGARET S; WINKLER WADE; BARRICK JEFFREY E; WICKISER JOHN K; UNIV YALE 摘要:It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural “riboswitchesâ€? (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies. In addition, the architecture of riboswitches allows actual pieces of the natural switches to be used to construct new non-immunogenic genetic control elements, for example the aptamer (molecular recognition) domain can be swapped with other non-natural aptamers (or otherwise modified) such that the new recognition domain causes genetic modulation with user-defined effector compounds. The changed switches become part of a therapy regimen—turning on, or off, or regulating protein synthesis. Newly constructed genetic regulation networks can be applied in such areas as living biosensors, metabolic engineering of organisms, and in advanced forms of gene therapytreatments.
专利号:WO-0231176-A1 优先权日:2000-10-12 标题:Process for producing nucleoside 发明人:FUJIWARA JUNYA; KOMATSU HIRONORI; AWANO HIROKAZU; FUKAZAWA NOBUYUKI; ANDO TOMOYUKI; TSUCHIYA KATSUTOSHI; CHIBA KYOKO; UMETANI HIDEKI; ARAKI TADASHI; YAMAUCHI TAKAHIRO 权利人:MITSUI CHEMICALS INC; FUJIWARA JUNYA; KOMATSU HIRONORI; AWANO HIROKAZU; FUKAZAWA NOBUYUKI; ANDO TOMOYUKI; TSUCHIYA KATSUTOSHI; CHIBA KYOKO; UMETANI HIDEKI; ARAKI TADASHI; YAMAUCHI TAKAHIRO 摘要:An anomer mixture of a nonnatural 1-phosphorylated saccharide is reacted with a base by the action of phosphorylase activity, wherein the exchange reaction between the phosphate group of the 1-phosphorylated saccharide and the base is conducted anomer-selectively. Metal cations capable of forming a sparingly water-soluble salt with phosphate ions are caused to be present in the reaction mixture, whereby the phosphate ions which are a by-product of the reaction can be precipitated as a sparingly water-soluble salt and the reaction equilibrium can be shifted toward nucleoside synthesis. Thus, the yield of the target compound is heightened. By utilizing a difference in the rate of the exchange reaction, a mixture of optical isomers of the nucleoside can be obtained in which one of the isomers is contained in a higher proportion.
专利号:EP-1179598-B1 优先权日:1999-05-13 标题 :Process for producing nucleoside compound 发明人:NIKUMARU SEIYA; NAKAMURA TAKESHI 权利人:MITSUI CHEMICALS INC 摘要:In preparation of a nucleoside compound by reacting a pentose-1-phosphate and a nucleic acid base or its analogue in the presence of enzyme activity of nucleoside phosphorylase, a metal salt capable of forming a water-insoluble salt with phosphoric acid may be added to a reaction system to eliminate phosphoric acid, a byproduct, from the reaction system so that the equilibrium reaction can be shifted toward a direction for nucleoside synthesis, leading to an improved yield of the desired nucleoside compound.
[参考文献]: M Alice Carvalho, Et Al. Efficient Conversion Of 6-Cyanopurines Into 6-Alkoxyformimidoylpurines. Org Biomol Chem. 2004 Apr 7;2(7):1019-24. [参考文献]: Zadkiel Alvarez, Et Al. Testing Nucleoside Analogues As Inhibitors Of Bacillus Anthracis Spore Germination In Vitro And In Macrophage Cell Culture. Antimicrob Agents Chemother. 2010 Dec;54(12):5329-36.
合成参考文献
摘要:Zhou, M.; Qin, T., Science of Synthesis, (2020) , 512.