CAS: 19962-37-9; 2-Acetamido-6-Hydroxypurine

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CAS号112233-74-6 n2-acetyl-o6-(d... | CAS号105970-04-5 2-amino-1-[(2-m... | CAS号39809-25-1 喷昔洛韦 | CAS号374750-30-8 2'-C-甲基鸟苷 | CAS号19188-42-2 Benzoic acid,4-... | CAS号82410-32-0 更昔洛韦 | CAS号15373-27-0 6H-Purin-6-one,... | CAS号118-00-3 鸟苷 | CAS号75128-73-3 N2-乙酰基-9-(2-乙酰氧... | CAS号104227-86-3 泛昔洛韦USP相关物质A | CAS号104227-87-4 泛昔洛韦

鸟嘌呤置于水体系中,用 乙醇,N,N-二甲基乙酰胺 用作溶剂,化学反应生成N-2-乙酰鸟嘌呤
参考文献:2-Nucleobase-Substituted 4,6-Diaminotriazine Analogs: Synthesis And Anti-Cancer Activity In 5-Fluorouracil-Sensitive And Resistant Colorectal Cancer Cells
标题:2-Nucleobase-Substituted 4,6-Diaminotriazine Analogs: Synthesis And Anti-Cancer Activity In 5-Fluorouracil-Sensitive And Resistant Colorectal Cancer Cells
摘要:<标题="">背景:癌症仍然是全球第二大死因,而结直肠癌(crc)是第三大最常见的癌症类型. 大肠癌(crc)是第三大常见癌症.尽管癌症 疗法取得了重大进展,但目前对 Crc 的治疗效果仍不理想.此外,现有的 此外,5-氟尿嘧啶(5-Fu)等化疗药物的疗效也受到了 Crc 获得性抗药性的限制. 方法:在本研究中,我们提供了合成四种新型核酸类似物的创新方法. 类似物.同样,我们还描述了这些化合物对 5G 细胞增殖,迁移,聚集和粘附的影响,聚合和粘附的影响. 人 Crc 细胞.在这两种细胞类型中,我们合成的新型类似物都能以浓度和时间依赖性方式显著抑制细胞活力. 浓度和时间依赖性.这凸显了这些新型类似物的更高效力. 类似物.此外,这些化合物还抑制了两种细胞类型的迁移和粘附,同时促进了同型细胞-细胞-细胞之间的作用. 它们促进了同型细胞-细胞间的相互作用. 结果:这些变化反映在基质金属蛋白酶(mmp-2 和 Mmp-9)的下调.此外,我们的类似物在体内表现出了强大的抗血管生成活性. 结论:这些新型核酸类似物降低了血管内皮生长因子(vegf)和血管内皮生长因子(vegf)分泌水平. 生长因子(vegf)和一氧化氮(no)的分泌水平. 细胞中的血管内皮生长因子(vegf)分泌水平和一氧化氮(no)产生.总之,我们的数据凸显了我们的新 类似物对 Crc(包括 5-Fu 耐药型)的潜在化疗特性.
Doi:10.2174/0929867329666220914112042

专利信息

专利号:US-9884885-B2
优先权日:2009-05-18
标题:Synthesis of labile base protected-modified deoxy and modified ribo nucleosides, corresponding phosphoramidites and supports and their use in high purity oligonucleotide synthesis
发明人：SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P
权利人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P; CHEMGENES CORP
摘要:This invention relates to novel method of synthesis of RNA utilizing N-2-acetyl protected guanine as nucleoside base, nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides and RNA oligonucleotide synthesis. Our discovery using N-acetyl protected guanine as nucleoside base protecting group, which is significantly faster base labile protecting group, yet significantly more stable than commonly utilized-2-isobutyryl guanosine is a novel approach to obtain highest purity oligonucleotides. This approach is designed to lead to very high purity and very clean oligonucleotide, after efficient removal of the protecting groups, including acetyl group from guanine and to produce high purity therapeutic grade DNA oligonucleotides, RNA oligonucleotides, diagnostic DNA, diagnostic RNA for microarray platform. The deprotection of acetyl protecting groups of the natural deoxy and ribonucleosides occurs under substantially reduced time in contact with mild deprotection conditions such as mild bases, secondary amines for removal of such groups under such conditions would allows synthesis of various DNA and RNA of highest purity for diagnostics and therapeutic application. This approach is designed to lead to high purity large scale therapeutic grade oligonucleotide chimeras which consist of fluoro sugar modification in conjunction with deoxy nucleosides, ribonucleosides, modified base and modified sugar nucleosides. This approach is further designed to use acetyl guanine protecting group when other bases are sensitive nucleoside, and for use in oligo peptide synthesis and for support bound oligo nucleotides.

专利号:US-7189849-B2
优先权日:1997-02-10
标 题:Synthesis of acyclic nucleoside derivatives
发明人：LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY
权利人:MEDIVIR AB
摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

专利号:EP-1565469-A1
优先权日:2002-11-22
标题:Process for the synthesis of ganciclovir
发明人：BABU JAYACHANDRA SURESH; RAY PURNA CHANDRA; KUMAR YATENDRA; KHANDURI CHANDRA HAS
权利人:RANBAXY LAB LTD
摘要:The present invention relates to an industrial useful process for the synthesis of antiviral compound, ganciclovir.

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:US-6043364-A
优先权日:1996-02-22
标 题:Regiospecific process for synthesis of acyclic nucleosides
发明人：KUMAR ASHOKE; SINGH DHARMENDRA; WANI MUKESH JAGANNATH; JOSHI NARENDRA SRIRAM; THOMBRE PRAVIN SAHADEV; RAWAT AJAY SINGH
权利人:LUPIN LAB LTD
摘要:N-7 isomer of the formula is converted into a N-9 isomer of the formula by heating a suspension of the N-7 isomer in an alkylating agent of the formula

专利号:EP-1414822-B1
优先权日:2001-06-26
标题:Improved synthesis of branched acyclic nucleosides
发明人：JANSEN GERT
权利人:MEDIVIR AB
摘要:A method for the preparation of acyclic nucleosides such as valomaciclovir stearate comprising the acid hydrolysis of an intermediate of the formula II: where X is a leaving group or an optionally protected guanine moiety, R1 is a hydroxy protecting group or a -C(=O)C1-C22 alkyl ester group; R2 and R3 are independently lower alkyl or benzyl, or R2 and R3 taken together are -CH2CH2- or -CH2CH2CH2- or -CH2CH2CH2CH2-; to the corresponding aldehyde of the formula III: and the reduction of the aldehyde to the corresponding alcohol of the formula IV: by the addition of a borohydride or borane aldehyde reducing agent, characterised in that the borohydride or borane aldehyde reducing agent is introduced under acid conditions.