(N-methylcarbonyloxymethyl) imidazole | 129075-21-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (N-methylcarbonyloxymethyl) imidazole
• 英文别名: (acetoxymethyl)imidazole；Imidazol-1-ylmethyl acetate
• CAS: 129075-21-4
• 化学式: C₆H₈N₂O₂
• 分子量: 140.142
• InChiKey: IURCAEOEZFJQSJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  44.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  三聚甲醛 、 1-乙酰基咪唑 在 zinc(II) chloride 作用下， 以 乙腈 为溶剂， 反应 16.0h， 以72%的产率得到(N-methylcarbonyloxymethyl) imidazole
  参考文献：
  名称：

  1-咪唑基甲基酯的简单两步合成

  摘要：

  描述了一种新的1-咪唑基甲基酯的合成方法，该合成方法是从适当的羧酸通过咪唑化物中间体开始的。

  DOI：

  10.1002/jhet.5570270362

文献信息

• Inhibitors of prenyl-protein transferase
  申请人：——

  公开号：US20020010184A1

  公开（公告）日：2002-01-24

  The present invention comprises piperazinone-containing compounds which inhibit prenyl-protein transferases, including famesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.

  该发明涉及含有哌嗪酮类化合物，可抑制前列蛋白转移酶，包括法美基蛋白转移酶和戈楞基蛋白转移酶I型。这种治疗性化合物对癌症的治疗具有用处。
• [EN] INHIBITORS OF PRENYL-PROTEIN TRANSFERASE<br/>[FR] INHIBITEURS DE PRENYL-PROTEINE-TRANSFERASES
  申请人：MERCK & CO., INC.

  公开号：WO1999009985A1

  公开（公告）日：1999-03-04

  (EN) The present invention is directed to compounds which inhibit prenyl-protein transferases, farnesyl-protein transferase and geranylgeranyl-protein transferase type I, and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I and the prenylation of the oncogene protein RAS.(FR) L'invention concerne des composés qui inhibent les prényl-protéine-transférases, la farnésyl-protéine-transférase et la géranylgéranyl-protéine-transférase de type I, de même que la prénylation de la protéine oncogène Ras. L'invention concerne également des compositions chimiothérapeutiques renfermant les composés considérés, ainsi que des procédés permettant d'inhiber la farnésyl-protéine-transférase, la géranylgéranyl-protéine-transférase de type I et la prénylation de la protéine oncogène Ras.

  该发明涉及抑制异戊二烯基-蛋白质转移酶、法尼基-蛋白质转移酶和生长酰基-蛋白质转移酶I型以及癌基因蛋白Ras的异戊二烯基化的化合物。该发明还涉及含有该发明化合物的化疗组合物以及抑制法尼基-蛋白质转移酶、生长酰基-蛋白质转移酶I型和癌基因蛋白Ras的异戊二烯基化的方法。
• Carboline Derivatives Useful in the Inhibition of Angiogenesis
  申请人：MOON Young-Choon

  公开号：US20070281962A2

  公开（公告）日：2007-12-06

  In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.

  根据本发明，已经鉴定出了抑制VEGF转录后表达的化合物，并提供了它们的使用方法。在本发明的一个方面，提供了在抑制VEGF产生、抑制血管生成和/或治疗癌症、糖尿病视网膜病变或渗出性黄斑变性方面有用的化合物。在本发明的另一个方面，提供了使用本发明中的化合物抑制VEGF产生、抑制血管生成和/或治疗癌症、糖尿病视网膜病变或渗出性黄斑变性的方法。
• CARBOLINE DERIVATIVES USEFUL IN THE INHIBITION OF ANGIOGENESIS
  申请人：Moon Young-Choon

  公开号：US20100179132A1

  公开（公告）日：2010-07-15

  In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.

  根据本发明，已经鉴定出抑制VEGF在转录后表达的化合物，并提供了它们的使用方法。本发明的一方面提供了用于抑制VEGF生产、治疗实体肿瘤癌和减少血浆和/或肿瘤VEGF水平的化合物。本发明的另一方面提供了使用本发明中的化合物抑制VEGF生产、治疗癌症和减少血浆和/或肿瘤VEGF水平的方法。
• Bis (acyloxymethyl) imidazole Derivative
  申请人：THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK

  公开号：EP0313724A2

  公开（公告）日：1989-05-03

  This invention relates to new bis(acyloxymethyl)imidazole derivatives; to compositions comprising these derivatives: and to processes for their utility as fungicides, bactericides and as inhibitors of the growth of cancer, particularly solid tumor cancer, in warm blooded animals of the formula: wherein M is N < or R: each R, R', and R" are independently selected from hydrogen and Z substituted or unsubstituted alkyl, cycloalkyl, cycloalkenyi, alkenyl, aryl, and heterocyclic ring wherein said ring comprises at least one of oxygen, nitrogen, sulfur or silicon; provided that N < may form a Z substituted or unsubstituted heterocyclic, and R and R attached to the imidazole ring, may form a Z substituted or unsubstituted heterocyclic ring; X is selected from at least one of oxygen, sulfur, nitrogen and alkyl; provided further that silicon is not directly attached to oxygen, sulfur or nitrogen and R' is not hydrogen when X is oxygen or sulfur; and Z is selected from halogen, nitro, nitrile, alkyl, haloalkyl, alkenyl, carboxylic acid, carboxylic acid ester, carboxylic acid amide, ether, thioether, hydroxyl, acylated hydroxyl, sulfonylamide, sulfonylurea, sulfoxide, sulfone, substituted and unsubstituted amine or mixtures thereof.

  本发明涉及新的双(酰氧基甲基)咪唑衍生物；涉及包含这些衍生物的组合物；涉及它们作为杀真菌剂、杀细菌剂和作为癌症（尤其是实体瘤癌症）生长抑制剂在温血动物中的应用过程，其式如下： 其中 M 是 N < 或 R：每个 R、R'和 R "独立地选自氢和 Z 取代或未取代的烷基、环烷基、环烯基、烯基、芳基和杂环，其中所述环包括氧、氮、硫或硅中的至少一种；条件是 N < 可形成 Z 取代或未取代的杂环，而连接到咪唑环上的 R 和 R 可形成 Z 取代或未取代的杂环；X 选自氧、硫、氮和烷基中的至少一种；条件是硅不直接与氧、硫或氮相连，且当 X 为氧或硫时，R'不是氢；Z 选自卤素、硝基、腈、烷基、卤代烷基、烯基、羧酸、羧酸酯、羧酸酰胺、醚、硫醚、羟基、酰化羟基、磺酰酰胺、磺酰脲、亚砜、砜、取代和未取代的胺或它们的混合物。