其它别名Acyclovir Impurity 1/acyclovir Ep Impurity A/o-Acetyl Acyclovir/valaciclovir Ep Impurity I/2-[(2-Amino-6-Oxo-1,6-Dihydro-9H-Purin-9-yl)Methoxy]Ethyl Acetate; 9-(2'-Acetoxyethoxymethyl)-Guanine; Acyclovir Related Compound A (50 Mg) (2-[(2-Amino-6-Oxo-1,6-Dihydro-9H-Purin-9-yl)Methoxy]Ethyl Acetate); Acyclovir Impurity A; 9-[[2-(Acetyloxy)Ethoxy]Methyl]-2-Amino-1,9-Dihydro-6H-Purin-6-One; Aciclovir Impurity A (Pheur); Aciclovir Related Compound A (Usp); 2-[(2-Amino-6-Oxo-1,6-Dihydro-9H-Purin-9-yl)Methoxy]Ethyl Acetate
鸟嘌呤置于cesium Iodide Ammonium Sulfate体系中,用 乙腈 用作溶剂,化学反应 3.0H,反应生成9-(2-乙酰氧基乙氧基甲基)鸟嘌呤 参考文献:Efficient Synthesis Of Acyclic Nucleosides By N-Alkylation Of Pyrimidine And Purine-Bases Using A New Coupling Agent Of Cesium Iodide 标题:Efficient Synthesis Of Acyclic Nucleosides By N-Alkylation Of Pyrimidine And Purine-Bases Using A New Coupling Agent Of Cesium Iodide 摘要:成功合成了无环核苷,包括((1,3-双(苄氧基)-2-丙氧基)甲基)-2-硫代吡啶,-尿嘧啶,-2-硫代尿嘧啶和-2-硫代腺嘌呤,以及(2-乙酰氧乙氧基甲基)-2-硫代腺嘌呤,-2-硫代吡啶,-尿嘧啶和-2-硫代尿嘧啶,合成方法为在中性条件下,使用碘化铯在乙腈中通过与相应的烷基乙酸酯(2)和烷基氯化物(3)进行n-烷基化反应,获得了非常好的产量. Doi:10.1246/cl.1988.1045
专利信息
专利号:US-5496945-A 优先权日:1993-06-14 标题 :Process for the synthesis of 9-(2-hydroxyethoxy methyl) guanine 发明人:BRUZZESE TIBERIO; GUAZZI GIUSEPPE; ROGNONI MARCO; MARCON GIULIANO 权利人:SOLAR CHEM SA 摘要:A process for the synthesis of 9-(2-hydroxyethoxy methyl) guanine in which guanine, or its salts, is reacted with 2-4 moles of hexamethyldisilazane, in the presence of an aprotic solvent and of ammonium sulfate. Thereafter, the trimethylsilyl derivative, without being isolated, is reacted with a stoichiometric quantity of an acyloxyethoxy methyl halide and hydrolyzed with aqueous sodium acetate or sodium hydroxyde to give 9-(2-hydroxyethyoxy methyl) guanine.
专利号:US-5648489-A 优先权日:1994-05-17 标题 :Syntheses of acyclic guanine nucleosides 发明人:CHU CHUNG K; DU JINFA; WANG CHUNGUANG 权利人:UNIV GEORGIA 摘要:A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxy-ethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ('DHPG') where the N2,N9-diprotected guanine is reacted with CH3C(O)OCH2O(CH2)2)OC(O)CH3 or 2-acetoxymethoxy-1,3-diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.
专利号:WO-9941229-A1 优先权日:1998-02-11 标题:Halogenated phenyl alcohol amides (ligands of gabab receptor) having an anticonvulsant activity 发明人:CARVAJAL SANDOVAL GUILLERMO; MEZA TOLEDO SERGIO ENRIQUE 权利人:CARVAJAL SANDOVAL GUILLERMO; MEZA TOLEDO SERGIO ENRIQUE 摘要:New anticonvulsant compounds have been synthesized with a chlorine or fluorine atom in the position para of the phenyl ring. These compounds include DL-2-hydroxy-2-(4'-chlorophenyl)butyramide, DL-2-hydroxy-2-(4'-fluorophenyl)butyramide, DL-3-hydroxy-3-(4'-chlorophenyl)pentanamide, DL-3-hydroxy-3-(4'-fluorophenyl)pentanamide, DL-4-hydroxy-4-(4'-chlorophenyl)hexanamide and DL-4-hydroxy-4-(4'-fluorophenyl)hexanamide. Said compounds have a rather significant anticonvulsant activity against convulsions produced by pentylene tetrazol, as well as unexpected properties in particular a high affinity to the GABAB receptor in addition to a sustained anticonvulsant activity. The invention also relates to methods for the synthesis of halogenated phenyl alcohol amides such as indicated in the examples given in the disclosure.
专利号:US-5565565-A 优先权日:1994-08-04 标题 :Preparation of N-9 substituted guanine compounds 发明人:LODEWIJK ERIC; HAN YEUN-KWEI; SCHLOEMER GEORGE C; NGUYEN SAM L 权利人:SYNTEX INC 摘要:The invention relates to efficient and selective processes for the synthesis of the antiviral N-9 substituted guanine compounds acyclovir and ganciclovir.
专利号:RU-2111967-C1 优先权日:1996-09-26 标题:Method of synthesis of aciclovir
专利号:DE-69409578-T2 优先权日:1993-06-14 标 题:Process for the synthesis of 9- (2-hydroxyethoxymethyl) guanine
参考文献:10.1021/jm0308747 摘要:Prekupec S, Svedruzić D, Gazivoda T, Mrvos-Sermek D, Nagl A, Grdisa M, Pavelić K, Balzarini J, De Clercq E, Folkers G, Scapozza L, Mintas M, Raić-Malić S. Synthesis and biological evaluation of iodinated and fluorinated 9-(2-hydroxypropyl) and 9-(2-hydroxyethoxy)methyl purine nucleoside analogues. J Med Chem. 2003 Dec 18;46(26):5763–72. doi: 10.1021/jm0308747.