羟胺乙酸盐 | 22606-42-4

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 羟胺乙酸盐
• 英文名称: hydroxylamine acetate
• 英文别名: hydroxylammonium acetate；Hydroxylamine, acetate (salt)；acetic acid;hydroxylamine
• CAS: 22606-42-4
• 化学式: C₂H₃O₂*H₄NO
• 分子量: 93.0825
• InChiKey: HMNQNULAYXDEEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.57
• 重原子数：
  6
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  83.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  羟胺乙酸盐 生成 乙酰氧肟酸
  参考文献：
  名称：

  Jones, L. W.; Oesper, R., American Chemical Journal, 1909, vol. 42, p. 519

  摘要：

  DOI：
• 作为产物：
  描述：

  sodium acetate 在 盐酸羟胺 作用下， 以 水 为溶剂， 以98%的产率得到羟胺乙酸盐
  参考文献：
  名称：

  容易获得三组分形式的复杂Fe（III）的环状异羟肟酸。

  摘要：

  环状异羟肟酸可以看作是可溶性铁的有效结合剂，因此可以用作用于治疗铁超负荷疾病的化合物的有用部分。或者，它们是细菌铁载体（除铁代谢物）的类似物，可用于设计靶向递送的抗生素构建体。高邻苯二甲酸的Castagnoli-Cushman反应的一种较早描述的三组分变体（通过原位环脱水成相应的酸酐）扩展为使用羟胺代替反应的胺组分。使用乙酸羟胺和O-苄基羟胺是该转化成功的关键，因为试剂在回流甲苯中的溶解度更高（与盐酸盐相比）。发现开发的方案适合于N-羟基-和N-（苄氧基）四氢异喹啉酸的数克级合成。经测试，以新开发的形式合成的环状异羟肟酸是有效的Fe3 +配体，这使其成为上述应用的合适候选物。

  DOI：

  10.3390/molecules24050864
• 作为试剂：
  描述：

  胞苷 在 羟胺乙酸盐 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 50.0h， 生成 莫那比拉韦
  参考文献：
  名称：

  从胞苷到MK-4482（EIDD-2801）的简明路线

  摘要：

  到MK-4482（EIDD-2801，A两步路线1）的开发是由酯化和胞苷的hydroxamination的。选择性酰化和直接胺化消除了对保护基团和活化基团的需要，总收率为75％，比报道的17％的收率有明显提高。步骤数从五个转换减少到两个，并且将昂贵的尿苷替换为更多可用的胞苷。

  DOI：

  10.1039/d0cc05944g

文献信息

• N-Pyruvoyl-dl-phenylalanyl-dl-prolin-lactam. Über das thermische Abbauprodukt von Ergotamin
  作者：C. A. Grob、W. Meier

  DOI：10.1002/hlca.19560390319

  日期：——

  The thermal cleavage product C17H18O4N2 of ergotaniine is shown to be an optically active form of N-pyruvoyl-phenylalanine-proline laetam (Ia), the inactive form of which has been synthesized. So far attempts to synthesize compounds related to ergotamine of type V by addition of amides to Ia have been unsuccessful.

  麦角胺碱的热裂解产物C 17 H 18 O 4 N 2被显示为N-丙酮酰-苯丙氨酸-脯氨酸莱坦（Ia）的旋光形式，其非活性形式已被合成。迄今为止，通过向Ia中添加酰胺来合成与V型麦角胺有关的化合物的尝试均未成功。
• 3 amino alkyl indoles for use in treating migraine
  申请人：Glaxo Group Limited

  公开号：US04636521A1

  公开（公告）日：1987-01-13

  Compounds are disclosed of general formula (I) ##STR1## wherein R.sub.1 represents an alkyl, cycloalkyl, aryl or aralkyl group; R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sub.5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group; or R.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups; and physiologically acceptable salts, solvates and bioprecursors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients. Various processes for the preparation of the compounds are disclosed including, for example, a process involving reaction of an aminoalkyl indole with a sulphonylating agent in order to introduce the --SO.sub.2 -- group at the 5-position on the indole nucleus.

  揭示了一般式(I)的化合物 ##STR1## 其中R.sub.1代表烷基、环烷基、芳基或芳基烷基；R.sub.2、R.sub.3、R.sub.4、R.sub.6和R.sub.7，可以相同也可以不同，每个代表氢原子或C.sub.1-3烷基；R.sub.5代表氢原子或烷基、环烷基、烯基或芳基烷基；或者R.sub.4和R.sub.5一起形成芳基烷基亚甲基团或者R.sub.4和R.sub.5与它们连接的氮原子一起形成饱和的单环5-至7-成员环；Alk代表含有两个或三个碳原子的烷基链，可以未经取代或通过不超过两个C.sub.1-3烷基取代；以及其生理上可接受的盐、溶剂和生物前体。这些化合物被描述为潜在用于治疗偏头痛，并且可以以常规方式制备为含有一种或多种药学上可接受的载体或赋形剂的药物组合物。揭示了各种制备这些化合物的方法，例如，涉及氨基烷基吲哚与磺酰化试剂反应以在吲哚核上的5位引入--SO.sub.2--基团的过程。
• Antiepidermal growth factor receptor antibodies augment cytotoxicity of chemotherapeutic agents on squamous cell carcinoma cell lines
  作者：Deanna Brown、Robert Wang、Paul Russell

  DOI：10.1016/s0194-5998(00)70148-3

  日期：2000.1

  Recent literature by Fan et al (1993) demonstrated that addition of cisplatin and monoclonal antibody to the epidermal growth factor receptor (EGFR MAb) of the human squamous cell carcinoma (SCC), A431, eradicated gross tumors in nude mice. To determine whether a combination of either cisplatin or 5‐fluorouracil (5‐FU) with EGFR MAb could affect an SCC other than the A431 tumor model, an assay using 2 human tongue SCC cell lines, BroTo and SCC‐25, was performed. Cells were pretreated with 1.25 μg/mL cisplatin or 10 μg/mL 5‐FU. After a 4‐hour incubation period, cisplatin‐treated cells were washed with phosphate‐buffered saline solution. Various concentrations of EGFR MAb were then added, and after a 24‐hour incubation period, an MTT cell growth assay was performed. SCC‐25 cells exhibited a greater decrease in growth with the addition of 16 nmol/L EGFR MAb to cisplatin compared with the cytotoxicity of cisplatin alone (P < 0.001). However, this combination did not produce similar results with BroTo cells (P > 0.05). The combination of EGFR MAb and 5‐FU produced a growth inhibition versus control (unexposed cells) in both cell lines (P < 0.05). These findings suggest the possible augmentation of the activity of chemotherapeutic agents, cisplatin and/or 5‐FU, with the addition of EGFR MAb on SCC cell lines other than A431. (Otolaryngol Head Neck Surg 2000;122:75‐83.)

  Fan 等人（1993 年）的最新文献表明，加入顺铂和表皮生长因子受体单克隆抗体（EGFR MAb）的人类鳞状细胞癌（SCC）A431 可根除裸鼠身上的肿瘤。为了确定顺铂或 5-氟尿嘧啶（5-FU）与表皮生长因子受体 MAb 结合使用是否会影响 A431 肿瘤模型以外的 SCC，研究人员使用 BroTo 和 SCC-25 这两种人类舌 SCC 细胞系进行了一项试验。用 1.25 μg/mL 顺铂或 10 μg/mL 5-FU 对细胞进行预处理。培养 4 小时后，用磷酸盐缓冲盐水洗涤顺铂处理过的细胞。然后加入不同浓度的表皮生长因子受体 MAb，培养 24 小时后，进行 MTT 细胞生长试验。与单独使用顺铂的细胞毒性相比，在顺铂中加入 16 nmol/L 表皮生长因子受体 MAb 的 SCC-25 细胞的生长下降幅度更大（P < 0.001）。然而，这种组合对 BroTo 细胞没有产生类似的结果（P >；0.05）。在两种细胞系中，表皮生长因子受体 MAb 和 5-FU 的组合与对照组（未暴露细胞）相比都产生了生长抑制作用（P < 0.05）。这些发现表明，在 A431 细胞系以外的 SCC 细胞系中添加表皮生长因子受体 MAb，可能会增强顺铂和/或 5-FU 等化疗药物的活性。(耳鼻咽喉头颈外科学 2000；122：75-83）。
• Myocardial Damage Induced by Uncontrolled Reoxygenation
  作者：Antonio F Corno、Giuseppina Milano、Michele Samaja、Ludwig K von Segesser

  DOI：10.1177/021849230000800109

  日期：2000.3

  To evaluate myocardial impairment induced by uncontrolled reoxygenation, the effects of hypoxia-reoxygenation were compared with ischemia-reperfusion in isolated rat hearts. After stabilization, 2 groups (n = 8) of Langendorff-perfused rat hearts were exposed to 40 minutes of ischemia (10% of baseline flow) or hypoxia (10% of baseline oxygen content) followed by a sudden return to baseline conditions (reperfusion or reoxygenation). The O₂ content was identical for the two groups during baseline conditions, O₂ shortage, and O₂ readmission. Metabolic (lactate production) and functional parameters (heart rate, peak systolic pressure, left ventricular developed pressure, maximal contraction and relaxation rates, end-diastolic pressure, coronary perfusion pressure) were recorded at the end of stabilization, after O₂ deficiency, and after 2 minutes of reoxygenation. Systolic function was significantly depressed after ischemia (p < 0.0001) but completely recovered to baseline values after 2 minutes of reperfusion. In contrast, systolic function was less severely depressed after hypoxia but failed to return to baseline after 2 minutes of reoxygenation. Diastolic function, unchanged during ischemia-reperfusion, remained significantly impaired during hypoxia-reoxygenation.

  为了评估未受控制的再氧化引起的心肌损伤，将缺氧再氧化的影响与离体大鼠心脏的缺血再灌注进行比较。稳定后，将2组Langendorff灌注的大鼠心脏（n=8）暴露于40分钟的缺血（基线流量的10%）或缺氧（基线氧含量的10%），然后突然返回基线条件（再灌注或再氧化）。在基线条件、氧缺乏和氧重新供应期间，两组的O2含量是相同的。代谢（乳酸产生）和功能参数（心率、峰值收缩压、左心室发育压力、最大收缩和松弛速率、舒张末压力、冠状动脉灌注压）在稳定后、O2缺乏后和2分钟再氧化后记录。收缩功能在缺血后明显受损（p <0.0001），但在2分钟再灌注后完全恢复到基线值。相反，收缩功能在缺氧后受损较轻，但在2分钟再氧化后未能恢复到基线。舒张功能在缺血再灌注期间未改变，在缺氧再氧化期间仍然明显受损。
• Process for the preparation of hydroxamic acid derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US06452010B1

  公开（公告）日：2002-09-17

  The present invention provides an improved process for preparing an hydroxycarbamoyl derivative of a carboxylic acid using a hydroxylammonium salt of a carboxylic acid as a reagent.

  本发明提供了一种改进的制备羧酸的羟基氨基甲酰衍生物的方法，使用羧酸的羟胺盐作为试剂。