(2-methyl-6-oxo-1,6-dihydro-pyrimidin-5-yl)-acetic acid ethyl ester | 14273-42-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: (2-methyl-6-oxo-1,6-dihydro-pyrimidin-5-yl)-acetic acid ethyl ester
• 英文别名: (2-Methyl-6-oxo-1,6-dihydro-pyrimidin-5-yl)-essigsaeure-aethylester；ethyl 2-(2-methyl-6-oxo-1H-pyrimidin-5-yl)acetate
• CAS: 14273-42-8
• 化学式: C₉H₁₂N₂O₃
• 分子量: 196.206
• InChiKey: PRAINMVCYZHQED-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  67.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (2-methyl-6-oxo-1,6-dihydro-pyrimidin-5-yl)-acetic acid ethyl ester 在 盐酸 、 sodium hydroxide 、 sodium hypochlorite 、 氨 、 水 、 氢溴酸 、 溶剂黄146 、 sodium nitrite 作用下， 生成 羟基硫胺素盐酸盐
  参考文献：
  名称：

  Use of Muscle Functional Magnetic Resonance Imaging With Older Individuals

  摘要：

  Muscle functional magnetic resonance imaging (mfMRI) has been widely used to study muscle recruitment in exercise in young healthy subjects, but has not been validated or used with older subjects. This study validates and demonstrates the use of mfMRI in older subjects. Subjects consisted of apparently healthy sedentary younger (n = 7) and older (n = 6) women. Proton transverse relaxation (T2)-weighted MRI scans were obtained of the quadriceps femoris at rest and immediately following three bouts of knee extension exercise (50%, 75%, and 100% of untrained 5 x 10 repetition maximum [RM]). Older subjects performed knee extension training for 12 weeks and repeated the MRI scan protocol using the same absolute loads. Training induced a 13% increase in 1 RM and a 25% increase in 5 x 10 RM. Older subjects had higher resting T2 values compared with younger subjects; however, the T2 response to exercise (slope) was similar among groups (young = 0.063 +/- 0.003, older untrained = 0.055 +/- 0.011, older trained = 0.053 +/- 0.008; p > .05). In all cases, T2 increased Linearly with load. Trained older subjects showed a lower T2 response when lifting the same absolute load compared with before training, which is consistent with results previously obtained from young subjects. In the older population, mfMRI is appropriate for use and offers benefits over other technologies.

  DOI：

  10.1093/gerona/55.10.b504
• 作为产物：
  描述：

  (2-methyl-6-oxo-1,6-dihydro-pyrimidin-5-yl)-acetic acid 在 盐酸 作用下， 生成 (2-methyl-6-oxo-1,6-dihydro-pyrimidin-5-yl)-acetic acid ethyl ester
  参考文献：
  名称：

  DE670095

  摘要：

  公开号：

文献信息

• Convenient synthesis of 2-substituted 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones
  作者：Eszter Kókai、József Nagy、Tünde Tóth、József Kupai、Péter Huszthy、Gyula Simig、Balázs Volk

  DOI：10.1007/s00706-015-1634-1

  日期：2016.4

  AbstractA new synthetic route was elaborated at our laboratory providing a convenient access to 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones (diazaoxindoles), a compound family of biological relevance. Treatment of the easily available ethyl 2-(4-chloropyrimidin-5-yl)acetate derivatives with ammonia afforded the corresponding 2-(4-aminopyrimidin-5-yl)acetamides, which were finally cyclized to the

  摘要在我们的实验室精心设计了一条新的合成路线，可方便地获得5,7-dihydro-6 H -pyrrolo [2,3- d ] pyrimidin-6-ones（diazaoxindoles），这是一种具有生物相关性的化合物。用氨处理易于获得的2-（4-氯嘧啶-5-基）乙酸乙酯衍生物，得到相应的2-（4-氨基嘧啶-5-基）乙酰胺，其最终环化为目标化合物。 图形概要
• Oxindolylquinazoline derivatives as angiogenesis inhibitors
  申请人：Zeneca Limited

  公开号：US06294532B1

  公开（公告）日：2001-09-25

  The invention relates to compounds of formula (I) and salts thereof as further defined herein, wherein ring Z is a 6-membered heterocyclic ring containing 1 to 3 nitrogen atoms, and the use of such compounds and salts to inhibit the effects of VEGF and FGF, and in the treatment of a number of disease states including cancer and rheumatoid arthritis.

  该发明涉及公式（I）的化合物及其盐，如本文所进一步定义的，其中环Z是含有1至3个氮原子的6元杂环环，以及利用这些化合物和盐来抑制VEGF和FGF的作用，并用于治疗包括癌症和类风湿性关节炎在内的多种疾病状态。
• COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
  申请人：ASANA BIOSCIENCES, LLC

  公开号：US20160222014A1

  公开（公告）日：2016-08-04

  The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.

  本申请提供了新型的可选取代的融合吡啶和嘧啶双环化合物及其药学上可接受的盐。还提供了制备这些化合物的方法。通过向受试者注射一种或多种化合物的治疗有效量，这些化合物有助于共同调节FAK和/或Src活性。通过这样做，这些化合物对治疗与FAK和/或Src通路失调相关的疾病有效。有利的是，这些化合物作为双重FAK和/或Src抑制剂发挥作用。这些化合物可用于治疗多种疾病，包括以炎症或异常细胞增殖为特征的疾病。在一种实施方式中，疾病是癌症。
• Treatment‐Mediated Changes in Human Immunodeficiency Virus (HIV) Type 1 RNA and CD4 Cell Counts as Predictors of Weight Growth Failure, Cognitive Decline, and Survival in HIV‐Infected Children
  作者：Jane C. Lindsey、Michael D. Hughes、Ross E. McKinney、Mary K. Cowles、Janet A. Englund、Carol J. Baker、Sandra K. Burchett、Mark W. Kline、Andrea Kovacs、Jack Moye

  DOI：10.1086/315865

  日期：2000.11

  This meta-analysis of 5 large studies of the Pediatric AIDS Clinical Trials Group was undertaken to evaluate the predictive value of antiretroviral treatment-mediated changes in 3 markers of human immunodeficiency virus (HIV) type 1 disease progression—HIV-1 RNA level, CD4 cell count, and CD4 percentage—for weight growth failure, cognitive decline, and survival in HIV-infected children. Proportional hazards models were used to assess the prognostic value of the markers at baseline and after 24 weeks of treatment, with data from 1089 children. Among children receiving nucleoside with or without nonnucleoside reverse-transcriptase inhibitors, higher immunologic and lower virologic markers at baseline and after 24 weeks were significant independent predictors of survival, whereas virologic markers were significant predictors of weight growth and cognitive failure in children >1 year old. The finding of differential age effects on pediatric-specific clinical outcomes emphasizes the need for continued investigation of treatment effects in children.

  本研究对儿科艾滋病临床试验组的 5 项大型研究进行了荟萃分析，以评估抗逆转录病毒治疗介导的人类免疫缺陷病毒（HIV）1 型疾病进展的 3 个指标--HIV-1 RNA 水平、CD4 细胞计数和 CD4 百分比的变化对 HIV 感染儿童体重增长失败、认知能力下降和存活率的预测价值。我们使用比例危险模型评估了这些指标在基线和治疗 24 周后的预后价值，数据来自 1089 名儿童。在接受核苷类与非核苷类逆转录酶抑制剂治疗的儿童中，基线和24周后较高的免疫学指标和较低的病毒学指标是生存率的重要独立预测因素，而病毒学指标则是体重增长和1岁以上儿童认知功能衰竭的重要预测因素。对儿童特异性临床结果的不同年龄影响的发现强调了继续研究儿童治疗效果的必要性。
• Andersag; Westphal, Chemische Berichte, 1937, vol. 70, p. 2035,2044
  作者：Andersag、Westphal

  DOI：——

  日期：——