CAS: 17902-23-7; 5-Fluoro-1-(Tetrahydrofuran-2-yl)Pyrimidine-2,4(1H,3H)-Dione

该化合物是一种五氟聚氨酯衍生物,具有增强稳定性和改善生物利用率的作用. 它的主要优势在于它相对于其母体化合物的威力增加,可以降低剂量,减少副作用,同时保持治疗效力. 它在各种临床环境中被用作抗癌剂.

结构式图片

相似化合物

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CAS号1191-99-7 2,3-二氢呋喃 | CAS号51-21-8 5-氟尿嘧啶 | CAS号75-78-5 二甲基二氯硅烷 | CAS号110-89-4 六氢吡啶 | CAS号65906-07-2 1-(2-tetrahydro... | CAS号7440-44-0 活性炭 | CAS号65906-08-3 5-fluoro-1-(2-t... | CAS号13369-70-5 2-氯四氢呋喃 | CAS号58138-78-6 5-氟-2,4-双(三甲硅氧)嘧啶 | CAS号1336-21-6 氨水 | CAS号51-21-8 5-氟尿嘧啶 | CAS号109-99-9 四氢呋喃 | CAS号110-00-9 呋喃 | CAS号68723-23-9 dehydroftorafur | CAS号66067-15-0 cis-1-[4-hydrox... | CAS号66067-14-9 1-(3-hydroxytet... | CAS号55185-82-5 5-fluoro-1,3-bi... | CAS号82178-07-2 N1-(2-furanidyl...

合成工艺路线路线简述

  • 合成目标产物 Tegafur 主要起始原料 Tetrahydrofuran And 5-Fluorouracil
  • (文献来源)合成步骤主要原料 Tetrahydrofuran 和 5-Fluorouracil
1,3-二(四氢-2-呋喃基)-5-氟尿嘧啶置于水体系中,用 乙醇 用作溶剂,化学反应 2.0H,以76%的收率获得替加氟
参考文献:一种抗肿瘤药物替加氟的制备方法
标题:一种抗肿瘤药物替加氟的制备方法
摘要:本发明属于有机合成化学领域,具体涉及一种抗肿瘤药物替加氟的制备方法.本发明以5‑氟尿嘧啶和四氢呋喃为原料,加过氧化物,催化剂四烷基碘化铵盐和碱,就能高效合成替加氟.该方法无需无水无氧,高温高压等苛刻条件,不需用到有毒物料与金属催化剂,且物料廉价易得,利于工业化生产.

海关参考信息

专利信息


专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

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:US-5075446-A
优先权日:1989-12-29
标题:Synthesis of tetrahydro-2-furylated pyrimidine derivatives
发明人:KIM YONG H; LEE CHUN H
权利人:KOREA ADVANCED INST SCI & TECH
摘要:The synthesis of 1-(tetrahydro-2-furyl) pyrimidine derivatives in good yields by the reaction of trimethylsilylated pyrimidine bases with 2-acetoxytetrahydrofuran using a catalytic amount of cesium chloride in acetonitrile under mild conditions is described.

专利号:US-2024209029-A1
优先权日:2021-04-21
标题:Adiponectin glycopeptides and compositions and methods of use thereof
发明人:WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN
权利人:UNIV HONG KONG
摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.
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主要参考文献


1: Kim J, Kim SH, Lee MG, Chung KY, Kim DS. Eccrine Squamous Syringometaplasia of Underlying Syringoma Associated with Tegafur/Gimeracil/Oteracil (TS-1). Acta Derm Venereol. 2015 Mar 13. doi: 10.2340/00015555-2092. [Epub ahead of print] doi: 10.1016/j.lungcan.2014.10.013. Epub 2014 Nov 3. Japanese. Japanese. doi: 10.1111/jphp.12304. Epub 2014 Aug 13.

合成参考文献


摘要:Shimane T, Mori T, Ono T, Kaburagi A, Monden T, Furuya A, Kamakazu K, Kobayashi S, Sanbe T, Suzaki H. [Effectiveness of concomitant therapy with S-1, nedaplatin, and radiation for laryngeal cancer]. Gan To Kagaku Ryoho. 2010 Feb;37(2):241–4.
摘要:Ina K, Hibi S, Furuta R, Takeuchi Y, Nagao S, Kayukawa S, Masaki A, Kataoka T. [Combination therapy of S-1 and 24-h infusion of cisplatin after palliative gastrectomy for stage IV gastric cancer]. Gan To Kagaku Ryoho. 2010 Feb;37(2):251–4.
摘要:Teshima S, Saito T, Endo A, Yunome G, Harada A, Ooshio H, Kodama H, Takeda K, Kikuchi S. [Problems of adjuvant chemotherapy with S-1 for gastric cancer]. Gan To Kagaku Ryoho. 2010 Feb;37(2):255–8.
摘要:Taomoto J, Tanabe K, Suzuki T, Hamai Y, Emi M, Hihara J, Yoshida K, Okada M. [Adjuvant surgery for advanced gastric cancer]. Gan To Kagaku Ryoho. 2010 Feb;37(2):263–6.
摘要:Fujimoto H, Oyama T, Suito T, Hashimoto K, Kameyama Y, Yasuda H, Ishizuka H. [A case of complete response treated by S-1 with concurrent radiotherapy for a gefitinib-resistant non-small cell lung cancer patient]. Gan To Kagaku Ryoho. 2010 Feb;37(2):295–8.
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