CAS: 31698-14-3; (2R,3R,3As,9Ar)-2-(Hydroxymethyl)-6-Imino-2,3,3A,9A-Tetrahydro-6H-Furo[2',3':4,5]Oxazolo[3,2-A]Pyrimidin-3-Ol

该化合物是细胞碘的一种合成核素,主要因其在癌症治疗中的潜在用途而得到承认,它是一种抗除虫素,它干扰DNA合成和复制,模仿天然核素,其特点是它能够抑制酶核素核素脱氧酶,这对将核素核素转化为脱氧核素至关重要,从而破坏癌症细胞等迅速分裂细胞的扩散.Ancitabine通常在临床环境中进行,并研究其对抗各种恶性肿瘤的效果,其化学结构包括一种改良的糖细胞,与天然的同类相比,它能够增强它的稳定性和生物利用率.与许多乳腺化剂一样,使用Ancitabine可能与副作用有关,因此在治疗期间需要仔细监测.总的来说,Ancitabine是发展定向癌症疗法的一个重要领域.

结构式图片

上下游产品

CAS号10323-20-3 D-阿拉伯糖 | CAS号65-46-3 胞嘧啶核苷 | CAS号27963-98-0 O,N-Aminomethan... | CAS号58311-73-2 (Z)-(2-CYANOVIN... | CAS号55628-10-9 4-amino-1-((3aR... | CAS号74580-91-9 4-amino-1-((2R,... | CAS号1070-71-9 丙炔腈 | CAS号10212-20-1 2'-脱氧-2-氟胞苷 | CAS号147-94-4 阿糖胞苷 | CAS号80791-93-1 5-碘-2'-氟-脱氧胞苷

合成工艺路线路线简述

  • 合成目标产物 Ancitabine 主要起始原料 D-(-)-Arabinose
  • (文献来源)合成步骤主要原料 D-(-)-Arabinose
阿拉伯糖置于potassium Hydrogencarbonate体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成安西他滨
参考文献:An Efficient Synthesis Of 1-.Beta.-D-Arabinofuranosylcytosine
标题:An Efficient Synthesis Of 1-.Beta.-D-Arabinofuranosylcytosine
摘要:
Doi:10.1021/jo00872A032

海关参考信息

专利信息


专利号:EP-1108724-B1
优先权日:1996-01-16
标题 :Synthesis of methoxy nucleosides and enzymatic nucleic acid molecules
发明人:WINCOTT FRANCINE; BEIGELMANN LEONID; MATULIC-ADAMIC JASENKA; USMAN NASSIM; HAEBERLI PETER; KARPEISKY ALEXANDER; SWEEDLER DAVID; JARVIS THALE; DIRENZO ANTHONY
权利人:SIRNA THERAPEUTICS INC
摘要:This invention relates to chemical synthesis of 2'-O-methyl, 3'-O-methyl and 5'-O-methyl nucleosides, incorporation of novel chemical modifications in enzymatic nucleic acid molecules and improved methods for the synthesis of enzymatic nucleic acid molecules.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
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✅ COA系统入驻 | 共享模式

主要参考文献


1: Kirsch LE, Notari RE. Pharmacokinetic prodrug modeling: in vitro and in vivo kinetics and mechanisms of ancitabine bioconversion to cytarabine. J Pharm Sci. 1984 Jun;73(6):728-32.
7: Lee CC, Schrier WH, Nagyvary J. The enzymatic hydrolysis of the phosphate ester bond in some thionucleotides. Biochim Biophys Acta. 1979 Jan 26;561(1):223-31.
11: Hadfield AF, Sartorelli AC. The pharmacology of prodrugs of 5-fluorouracil and 1-beta-D-arabinofuranosylcytosine. Adv Pharmacol Chemother. 1984;20:21-67. Review. Review. Review.

合成参考文献


摘要:Eksperimental'naya i Klinicheskaya Farmakoterapiya., 9(31), 1980
摘要:Latysheva SV. [Comparative assessment of the effectiveness of antiviral agents used for the therapy of recurrent herpetic stomatitis]. Stomatologiia (Mosk). 1985 May;64(3):25–7.
参考文献:10.1016/0003-9969(93)90091-y
摘要:Proctor GB, Shori DK, Chan KM, Garrett JR. Asynchronous reformation of individual kallikrein-related secretory proteinases in rat submandibular glands following degranulation by cyclocytidine. Arch Oral Biol. 1993 Oct;38(10):827–35. doi: 10.1016/0003-9969(93)90091-y.
参考文献:10.1016/0306-3623(94)90033-7
摘要:Novotný L, Balážová E, Tejc P, Ujházy V. Effect of arabinosylcytosine derivative cyclocytidine on hepatal functions in rats and on Zajdela hepatoma. General Pharmacology: The Vascular System. 1994 Jan;25(1):201–4. doi: 10.1016/0306-3623(94)90033-7.
参考文献:10.1016/0003-9969(94)90176-7
摘要:Garrett JR, Thomopoulos GN, Zhang XS, Hartley R. The fate of glycogen in granular tubule cells of rat submandibular glands during secretory events. Arch Oral Biol. 1994 May;39(5):449–52. doi: 10.1016/0003-9969(94)90176-7.
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