CAS: 703-95-7; 5-Fluoro-2,6-Dioxo-1,2,3,6-Tetrahydropyrimidine-4-Carboxylic Acid

该化合物是分子生物学和遗传学中常用的,作为选择性制剂的微米类仿制药剂,是酵母遗传学中的一个关键工具,特别是用于抗选颗粒抖动和基因淘汰研究中的抗选工具. 5-FOA被URA3基因产品Orotidine-5'-磷酸酯脱碳基酶代谢为有毒化合物5-氟尿素,从而能够选择三氯硝基苯菌株,其高特性和效率使其对沙焦乐菌蛋白和其他模型生物的基因操纵具有宝贵价值,还用于研究核糖化生物合成和抗硫酸研究,因为其抑制对基新陈代谢作用.

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2-ethylsulfanyl-5-fluoro-6-oxo-1,6-dihydro-pyrimidine-4-carboxylic acid ethyl ester ethyl 2-(methylmercapto)-4-hydroxy-5-fluoro-6-pyrimidinecarboxylate 5-fluorouracil

合成工艺路线路线简述

    在 盐酸体系中,用 水 作为反应溶剂,化学反应 4.0H,以79%的收率获得产物5-氟乳清酸
    参考文献:一种絮凝剂添加物5-氟乳清酸的合成工艺
    标题:一种絮凝剂添加物5-氟乳清酸的合成工艺
    摘要:本发明公开的属于精细化工技术领域,具体为一种絮凝剂添加物5‑氟乳清酸的合成工艺,该絮凝剂添加物5‑氟乳清酸的合成工艺的具体步骤如下:S1:氟乙酸酯与草酸酯在碱性条件下发生缩合反应,缩合反应温度为0~50°C,反应时间为1~10小时;s2:步骤s1中缩合反应后的产物再与o‑甲基异脲盐发生环合反应得到2‑二甲氧基‑4‑羟基‑5‑氟‑6‑甲酸酯嘧啶;s3:2‑二甲氧基‑4‑羟基‑5‑氟‑6‑甲酸酯嘧啶与盐酸发生水解反应,得到5‑氟乳清酸.本方案提供了化合物5‑氟清乳酸的合成工艺路线,此工艺路线步骤短,操作简单,原料易得,成本低,易于纯化,适合工业化生产.

    海关参考信息

    专利信息


    专利号:US-7230101-B1
    优先权日:2002-08-28
    标 题:Synthesis of methotrexate-containing heterodimeric molecules
    发明人:MURTHI KRISHNA K; SMITH CHASE C
    权利人:GPC BIOTECH INC
    摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

    专利号:US-6818633-B2
    优先权日:2001-06-29
    标题:Antiviral compounds and methods for synthesis and therapy
    发明人:BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
    权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
    摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

    专利号:WO-2022080234-A1
    优先权日:2020-10-12
    标 题 :Method for modifying genome of algae belonging to genus galdieria
    发明人:KOKUBUN Yume; YAMASAKI HIROAKI; MIYAGISHIMA SHIN-YA; HIROOKA Shunsuke; FUJIWARA TAKAYUKI
    权利人:DAINIPPON INK & CHEMICALS; INTER UNIV RESEARCH INSTITUTE CORPORATION RESEARCH ORGANIZATION OF INFORMATION AND SYSTEMS
    摘要:Provided are: a method for modifying the genome of algae belonging to the genus Galdieria, comprising a step for carrying out genome modification on a haploid form of algae belonging to the genus Galdieria; a method for producing genome-modified algae belonging to the genus Galdieria, comprising a step for carrying out genome modification of algae belonging to the genus Galdieria using the genome modification method; a method for producing a desired substance or food, which uses algae belonging to the genus Galdieria obtained using the production method; and algae belonging to the genus Galdieria, that has a mutation in a gene that participates in the synthesis of a nutrient component and that has a requirement for the nutrient component.

    专利号:US-2025263763-A1
    优先权日:2020-08-27
    标 题 :Production of oxygenated diterpenoid compounds
    发明人:ANDERSEN-RANBERG JOHAN; HANSEN NIKOLAJ; FORMAN VICTOR
    权利人:UNIV COPENHAGEN
    摘要:Disclosed is a method for production of oxygenated diterpenoid compounds, such as triptophenolide, triptonide and triptolide, by inserting genes encoding particular cytochrome P450 enzymes and expressing the genes in selected host cells for synthesis of the compounds. Further disclosed are particular cytochrome P450 enzymes suitable for this synthesis.

    专利号:WO-2023164985-A1
    优先权日:2022-03-02
    标题 :Genetically engineered bacterium for synthesizing p-coumaric acid and derivative thereof, method for constructing same and use thereof
    发明人:YU TAO; LUO WEI; GUO SHUYUAN
    权利人:SHENZHEN INST OF ADV TECH CAS
    摘要:A genetically engineered bacterium for synthesizing p-coumaric acid and derivatives thereof, a method for constructing same and use thereof. The genetically engineered bacterium for synthesizing p-coumaric acid comprises a chassis strain into which a p-coumaric acid synthesis gene has been introduced, and the chassis strain has also been subjected to any one of or a combination of at least two of the following genetic modifications: (1) deleting aro8 and aro9; (2) deleting tdh1, tdh2, tdh3, and overexpressing GAPB; (3) deleting idh1 or idh2, and simultaneously overexpressing YHM2 and IDP2; (4) deleting pgi1, pfk1, or pfk2, and simultaneously overexpressing ZWF1, GND1, RPE1, RKI1, TKL1, and TAL1; (5) overexpressing POS5; or (6) deleting gdh2. Efficient synthesis of p-coumaric acid and derivatives thereof is realized.

    专利号:WO-2022043461-A1
    优先权日:2020-08-27
    标 题 :Production of oxygenated diterpenoid compounds
    发明人:ANDERSEN-RANBERG JOHAN; HANSEN NIKOLAJ; FORMAN VICTOR
    权利人:UNIV COPENHAGEN
    摘要:Disclosed is a method for production of oxygenated diterpenoid compounds, such as triptophenolide, triptonide and triptolide, by inserting genes encoding particular cytochrome P450 enzymes and expressing the genes in selected host cells for synthesis of the compounds. Further disclosed are particular cytochrome P450 enzymes suitable for this synthesis.
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    主要参考文献


    1: Nguyen KT, Ho QN, Do LTBX, Mai LTD, Pham DN, Tran HTT, Le DH, Nguyen HQ, Tran VT. A new and efficient approach for construction of uridine/uracil auxotrophic mutants in the filamentous fungus Aspergillus oryzae using Agrobacterium tumefaciens-mediated transformation. World J Microbiol Biotechnol. 2017 Jun;33(6):107. doi: 10.1007/s11274-017-2275-9. Epub 2017 May 2. doi: 10.1080/09168451.2017.1295800. Epub 2017 Mar 14. doi: 10.1186/s13068-016-0692-x. eCollection 2017.
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    合成参考文献


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    摘要:Toombs JA, Liss NM, Cobble KR, Ben-Musa Z, Ross ED. [PSI+] Maintenance Is Dependent on the Composition, Not Primary Sequence, of the Oligopeptide Repeat Domain. PLoS ONE. 2011 Jul 08;6(7):e21953. doi: 10.1371/journal.pone.0021953.
    参考文献:10.1007/s00294-011-0350-6
    摘要:Ruprich-Robert G, Wery M, Després D, Boulard Y, Thuriaux P. Crucial role of a dicarboxylic motif in the catalytic center of yeast RNA polymerases. Curr Genet. 2011 Oct;57(5):327–34. doi: 10.1007/s00294-011-0350-6.
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