6-aminomethyl-2-[tert-butyl(dimethylsilyloxy)methyl]pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 6-aminomethyl-2-[tert-butyl(dimethylsilyloxy)methyl]pyridine
• 英文别名: 2-aminomethyl-6-tert-butyldimethylsilyloxymethylpyridine；(6-(((tert-butyldimethylsilyl)oxy)methyl)pyridin-2-yl)methanamine；2-aminomethyl-6-[(tert-butyldimethylsilyloxy)methyl]pyridin；2-Aminomethyl-6-[(tert-butyldimethylsilyloxy)methyl]pyridine；[6-[[tert-butyl(dimethyl)silyl]oxymethyl]pyridin-2-yl]methanamine
• 化学式: C₁₃H₂₄N₂OSi
• 分子量: 252.432
• InChiKey: PSJBPIRAMIDKMH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.06
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-aminomethyl-2-[tert-butyl(dimethylsilyloxy)methyl]pyridine 在 4-二甲氨基吡啶 、 四丁基氟化铵 作用下， 以 四氢呋喃 、 吡啶 、 氘代氯仿 为溶剂， 反应 89.0h， 生成 4-[[6-[[[3-[[Bis(4-methoxyphenyl)-phenylmethoxy]methyl]phenyl]methylcarbamothioylamino]methyl]pyridin-2-yl]methoxy]-4-oxobutanoic acid
  参考文献：
  名称：

  AROMATIC COMPOUND, MODIFICATION CARRIER THAT USES SAME AND IS USED FOR SYNTHESIZING AN OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE DERIVATIVE, AND OLIGONUCLEOTIDE CONSTRUCT

  摘要：

  公开号：

  EP2511260B1
• 作为产物：
  描述：

  吡啶-2.6-二羧酸二甲酯 在 5%-palladium/activated carbon 锂硼氢 、 sodium azide 、 四溴化碳 、 氢气 、 sodium hydride 、 三乙胺 、 三苯基膦 作用下， 以 四氢呋喃 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 59.0h， 生成 6-aminomethyl-2-[tert-butyl(dimethylsilyloxy)methyl]pyridine
  参考文献：
  名称：

  AROMATIC COMPOUND, MODIFICATION CARRIER THAT USES SAME AND IS USED FOR SYNTHESIZING AN OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE DERIVATIVE, AND OLIGONUCLEOTIDE CONSTRUCT

  摘要：

  公开号：

  EP2511260B1

文献信息

• [EN] ADENOSINE RECEPTOR BINDING COMPOUNDS<br/>[FR] COMPOSÉS SE LIANT AU RÉCEPTEUR DE L'ADÉNOSINE
  申请人：NIKANG THERAPEUTICS INC

  公开号：WO2020014332A1

  公开（公告）日：2020-01-16

  The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.

  本发明涉及化学式（I）的药物化合物和组合物，以及使用这些化合物和组合物进行治疗的方法，特别是用于治疗和/或预防增殖性疾病，如癌症。如本文进一步描述的化合物（I）被显示为腺苷A2A受体的调节剂，并表现出抗增殖活性。因此，这些化合物对于治疗增殖性疾病如癌症以及其他与腺苷受体相关的疾病条件包括炎症性疾病、肾脏疾病、糖尿病、血管疾病、肺部疾病或自身免疫疾病是有用的。
• Cu²⁺and Pt²⁺complexes of pyrazole and triazole based dinucleating ligands
  作者：Alexander Eisenwiener、Markus Neuburger、Thomas A. Kaden

  DOI：10.1039/b612948j

  日期：——

  stability constants have been measured. The reactivity of the dinuclear species [Cu(2)LH(-1)] towards phosphate ester hydrolysis have shown that the OH-functionality incorporated in some of the ligands does not enhance the hydrolysis rate. Several ligands were reacted with Pt(2+) to give insoluble dinuclear species [Pt(2)LI(3)]. One of them was studied by X-ray diffraction and shows that the two Pt(2+) are

  合成了一系列吡唑和三唑基双核配体，并研究了它们对金属离子的络合潜力，并显示出方形的平面配位几何形状。在Cu（2+）的情况下，已使用pH滴定法确定了溶液中的络合平衡。已检测到化学计量比为1：1的物种[CuLH（n）]，化学计量比为2：1的物种[Cu（2）LH（m）]，并且具有二聚体性质的物种[Cu（2）L（2）H（p）]。并测量了它们的整体稳定性常数。双核物质[Cu（2）LH（-1）]对磷酸酯水解的反应活性表明，掺入某些配体中的OH-官能度不会提高水解速率。几个配体与Pt（2+）反应，生成不溶性双核物质[Pt（2）LI（3）]。其中一个通过X射线衍射进行了研究，结果表明两个Pt（2+）被吡唑基和一个I（-）桥接。其余两个位置被杂环的α位和末端I（-）的氨基占据。几乎是平面的[Pt（2）LI（3）]单元在晶体中形成薄片，相隔约4 A，因此指示pi堆积相互作用。
• Pyrimidine Compounds as Purine Receptor Antagonist
  申请人：Gillespie John Roger

  公开号：US20070281936A1

  公开（公告）日：2007-12-06

  Compounds of formula (I); wherein R 1 is H or NHZ; R 2 is optionally substituted aryl or heteroaryl attached via a carbon atom; R 3 is H; optionally substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or C 3 C 7 cycloalkyl, halogen; OH or OR, or R 4 is H, optionally substituted C 1 -C 6 alkyl, C 3 C 6 alkenyl, C 3 -C 6 alkynyl, C 3 -C 7 cycloalkyl, aryl or heteroaryl, R 5 is H or optionally substituted C 1 -C 6 alkyl, C 3 -C 6 alkenyl, C 3 -C 6 alkynyl, or C 3 -C 7 cycloalkyl; or R 4 and R 5 together form a 5 or 6-membered heterocyclic ring; and R 10 is optionally substituted C 1 -C 6 alkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease.

  化合物的公式（I）;其中R1是H或NHZ; R2是通过碳原子连接的可选取代芳基或杂环芳基; R3是H; 可选取代的C1-C6烷基，C2-C6烯基，C2-C6炔基或C3C7环烷基，卤素; OH或OR，或R4是H，可选取代的C1-C6烷基，C3C6烯基，C3-C6炔基，C3-C7环烷基，芳基或杂环芳基，R5是H或可选取代的C1-C6烷基，C3-C6烯基，C3-C6炔基或C3-C7环烷基; 或R4和R5一起形成5或6元杂环环; R10是可选取代的C1-C6烷基; 是嘌呤受体，特别是腺苷受体拮抗剂，用于治疗运动障碍，如帕金森病等。
• AROMATIC COMPOUND, MODIFICATION CARRIER THAT USES SAME AND IS USED FOR SYNTHESIZING AN OLIGONUCLEOTIDE DERIVATIVE, OLIGONUCLEOTIDE DERIVATIVE, AND OLIGONUCLEOTIDE CONSTRUCT
  申请人：Kitade Yukio

  公开号：US20120245341A1

  公开（公告）日：2012-09-27

  The present invention provides an oligonucleotide derivative that enables to easily synthesize an oligonucleotide derivative chemically modified at the 3′-end with two moieties each having a benzene or pyridine structure with a few steps, an aromatic compound serving as a precursor for preparing the modification carrier for synthesizing oligonucleotide derivative, and the oligonucleotide derivative and the oligonucleotide construct using the same, that is chemically modified at the 3′-end with two moieties each having a benzene or pyridine structure, and has good permeability through a cell membrane and excellent nuclease resistance. The modification carrier for synthesizing oligonucleotide derivative, comprising a unit and a carrier carrying the unit directly or via a linker, wherein the unit is represented by the formula (a): wherein, R 1 to R 6 each independently represent hydrogen or a substituent other than hydrogen; Z 1 and Z 2 each independently represent CH or nitrogen; and X represents oxygen or sulfur.

  本发明提供了一种寡核苷酸衍生物，使得可以通过几个步骤轻松地合成在3'-端带有两个苯或吡啶结构的化学修饰寡核苷酸衍生物，还提供了作为制备修饰载体的前体的芳香化合物，以及使用相同的化学修饰在3'-端带有两个苯或吡啶结构的寡核苷酸衍生物和寡核苷酸构建物，具有良好的细胞膜渗透性和出色的核酸酶抵抗性。用于合成寡核苷酸衍生物的修饰载体包括一个单元和一个携带该单元的载体，直接或通过连接剂携带该单元，其中该单元由式（a）表示：其中，R1到R6各自独立地表示氢或不是氢的取代基；Z1和Z2各自独立地表示CH或氮；X表示氧或硫。
• Pyrimidine compounds as purine receptor antagonist
  申请人：Vernalis (R&D) Limited

  公开号：US07875600B2

  公开（公告）日：2011-01-25

  Compounds of formula (I); wherein R1 is H or NHZ; R2 is optionally substituted aryl or heteroaryl attached via a carbon atom; R3 is H; optionally substituted C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, or C3 C7 cycloalkyl, halogen; OH or OR, or R4 is H, optionally substituted C1-C6alkyl, C3 C6alkenyl, C3-C6alkynyl, C3-C7 cycloalkyl, aryl or heteroaryl, R5 is H or optionally substituted C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, or C3-C7 cycloalkyl; or R4 and R5 together form a 5 or 6-membered heterocyclic ring; and R10 is optionally substituted C1-C6alkyl; are purine receptor, particularly adenosine receptor antagonists, useful for treatment of, inter alia, movement disorders such as Parkinsons disease.

  式(I)化合物，其中R1为H或NHZ；R2为通过碳原子连接的可选取代芳基或杂环芳基；R3为H；可选取代的C1-C6烷基，C2-C6烯基，C2-C6炔基或C3-C7环烷基，卤素；OH或OR，或R4为H，可选取代的C1-C6烷基，C3-C6烯基，C3-C6炔基，C3-C7环烷基，芳基或杂环芳基，R5为H或可选取代的C1-C6烷基，C3-C6烯基，C3-C6炔基或C3-C7环烷基；或R4和R5共同形成5或6成员杂环环；R10为可选取代的C1-C6烷基。这些化合物是嘌呤受体，特别是腺苷受体拮抗剂，可用于治疗运动障碍症，如帕金森病等。