5'-Brom-5'-deoxyuridin | 19556-55-9

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 5'-脱氧核糖核苷
• 英文名称: 5'-Brom-5'-deoxyuridin
• 英文别名: 5'-bromo-5'-deoxyuridine；5'-Desoxy-5'-brom-uridin；1-[(2R,3R,4S,5S)-5-(bromomethyl)-3,4-dihydroxyoxolan-2-yl]pyrimidine-2,4-dione
• CAS: 19556-55-9
• 化学式: C₉H₁₁BrN₂O₅
• 分子量: 307.101
• InChiKey: OLGIWRFTAFURRN-XVFCMESISA-N

物化性质

• 密度：
  1.901±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  99.1
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5'-Brom-5'-deoxyuridin 在 sodium thiosulfate 作用下， 以 乙醇 为溶剂， 反应 1.0h， 以52%的产率得到5'-Deoxyuridine-5'-S-thiosulfate sodium salt
  参考文献：
  名称：

  核苷 5'-S-硫代硫酸盐的合成与构象

  摘要：

  摘要 5'-溴-5'-脱氧-（或5'-甲苯磺酰基-）核苷与硫代硫酸钠反应生成各自的5'-S-硫代硫酸盐（核苷Bunte盐）。描述了新核苷酸类似物的构象和一些物理化学特性

  DOI：

  10.1515/znb-1998-1015
• 作为产物：
  描述：

  尿嘧啶核苷 在 四溴化碳 、 三苯基膦 作用下， 以 二氯甲烷 为溶剂， 以54%的产率得到5'-Brom-5'-deoxyuridin
  参考文献：
  名称：

  黑光诱导的环核苷酸的自由基环化方法：一种独立的方法。

  摘要：

  本文着重介绍了一种基于连续自由基反应制备环核苷衍生物的有效方法。反应在新颖的和常规的引发条件范围内，使用常见且有效的自由基氢供体，在有机和水性介质中进行，以提供良好至优异产率的相应环核苷。还讨论了转换的机械方面。

  DOI：

  10.2174/157017811795685108

文献信息

• Studies on Nucleosides and Nucleotides. VIII. Preparation and Reactions of Triphenylphosphoranediylnucleosides
  作者：Junji Kimura、Kentaro Yagi、Hideyuki Suzuki、Oyo Mitsunobu

  DOI：10.1246/bcsj.53.3670

  日期：1980.12

  The reaction of uridine, N4-benzoylcytidine, guanosine, and N6-p-toluoyladenosine with diethyl azodicarboxylate and triphenylphosphine resulted in the formation of the corresponding 2′,3′-O-(triphenylphosphoranediyl)-cyclonucleosides. On the other hand, adenosine afforded, under similar conditions, 3′,5′-O-(triphenylphosphoranediyl)adenosine (19). The difference can be explained in terms of the acidity

  尿苷、N4-苯甲酰胞苷、鸟苷和 N6-对甲苯酰腺苷与偶氮二羧酸二乙酯和三苯基膦的反应导致形成相应的 2',3'-O-（三苯基正膦二基）-环核苷。另一方面，在类似条件下，腺苷可提供 3',5'-O-（三苯基正膦二基）腺苷 (19)。这种差异可以用核苷碱基部分的酸度来解释。2',3'-O-(三苯基正膦二基)-O2,5'-环尿苷，N4-苯甲酰基-2',3'-O-(三苯基正膦二基)-O2,5'-环胞苷，2',3'的反应-O-(三苯基正膦二基)-N3,5'-环鸟苷或N6-p-toluoyl-2',3'-O-(三苯基正膦二基)-N3,5'-环腺苷与亲核试剂和亲电试剂添加相应的核苷衍生物游离的 2'-和 3'-羟基。因此 2', 3'-O-三苯基正膦二基作为保护基团，在反应产物的后处理过程中很容易去除。19与异氰酸苯酯反应制...
• Blood Concentrations of Amitriptyline and Its Metabolite in Rats after Acute Oral Administration of Amitriptyline
  作者：Seung-Kyung Baeck、Mie-Ae Lim、Seh-Youn Park、Ju-Seon Lee、Han-Sun Lee、Ki-Ser Koo

  DOI：10.1093/jat/24.4.271

  日期：2000.5.1

  Amitriptyline (AMT), a tricyclic antidepressant that is a dibenzocycloheptadine derivative, is frequently used. However, the case reports of AMT-related fatalities are increased, nowadays, due to the low levels of toxic and fatal concentration in blood. So, this study was carried out to determine the concentrations of AMT and its demethylated metabolite, nortriptyline (NTR), after acute single oral administration of AMT in rats. Blood samples were collected five times from the opthalmic venous plexus at 0, 1, 2, 4, and 8 h after acute single oral administration of AMT in toxic doses of 10 (Group I) or 20 mg/kg (Group II), and the concentrations of AMT and NTR and the mean ratios of AMT to NTR (AMT/NTR) in the blood were periodically determined at designated times. The blood concentrations of AMT and NTR were identified and quantitated by gas chromatography with thermionic specific detection and gas chromatography-mass spectrometry after solid-phase extraction with a Clean Screen DAU column. The peak blood concentrations of AMT and NTR in Group I were 0.34 and 0.28 µg/mL, respectively, and those of AMT and NTR in Group II were 0.59 and 0.43 µg/mL, respectively, and were reached at 1 h after single oral administration.

  阿米替林 (AMT) 是一种三环类抗抑郁药，是二苯并环庚啶衍生物，经常使用。然而，由于血液中有毒和致命浓度水平较低，如今与 AMT 相关的死亡病例报告有所增加。因此，本研究旨在测定大鼠急性单次口服 AMT 后 AMT 及其去甲基化代谢物去甲替林 (NTR) 的浓度。急性单次口服 AMT 中毒剂量 10（组 I）或 20 mg/kg（组 II）后，分别在 0、1、2、4 和 8 小时从眼部静脉丛采集 5 次血样，并在指定时间定期测定血液中AMT和NTR的浓度以及AMT与NTR的平均比率（AMT/NTR）。使用 Clean Screen DAU 柱进行固相萃取后，通过气相色谱法和热离子特异性检测以及气相色谱-质谱法对 AMT 和 NTR 的血液浓度进行鉴定和定量。 I组AMT和NTR的血峰浓度分别为0.34和0.28μg/mL，II组AMT和NTR的血峰浓度分别为0.59和0.43μg/mL，且在单次口服后1小时达到。
• Functional Immunohistochemical Cell Cycle Analysis as a Prognostic Indicator for Cancer
  申请人：Chen-Kiang Selina

  公开号：US20070212736A1

  公开（公告）日：2007-09-13

  The present invention relates to a method of determining the presence of a retinoblastoma protein (Rb)-mediated cancerous or pre-cancerous condition in a sample of fixed cells that involves exposing the sample to an antibody that recognizes phosphorylation of serine on the retinoblastoma protein (pS-Rb), and identifying cells in the sample that are recognized by the anti-O body to pS-Rb, where the recognition of pS-Rb in the sample determines the presence of an Rb-mediated cancerous or pre-cancerous condition. The method also involves identifying the presence of specific cell cycle markers and positive and negative cell cycle regulators to assess the stage of disease progression in a cancer patient having an (Rb)-mediated cancer. The present invention also relates to methods of assessing the efficacy of cancer therapy for an Rb-mediated cancer, determining the mechanism of cell cycle progression in an Rb-mediated cancer, and identifying cells predisposed to developing an Rb-mediated cancerous condition.
• US8603763B2
  申请人：——

  公开号：US8603763B2

  公开（公告）日：2013-12-10
• USRE46379E1
  申请人：——

  公开号：USRE46379E1

  公开（公告）日：2017-04-25