2-cyanoethyltetraisopropylphosphoramidite | 170158-27-7

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-cyanoethyltetraisopropylphosphoramidite
• 英文别名: 3-[[4,6-Dimethyl-1,3-di(propan-2-yl)-1,3,2-diazaphosphinan-2-yl]oxy]propanenitrile
• CAS: 170158-27-7
• 化学式: C₁₄H₂₈N₃OP
• 分子量: 285.37
• InChiKey: AJYGOQOLKBEWJW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  39.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-cyanoethyltetraisopropylphosphoramidite 、 在 4,5-二氰基咪唑 作用下， 以 二氯甲烷 为溶剂， 反应 0.5h， 以100%的产率得到
  参考文献：
  名称：

  Trapping and Structural Elucidation of a Very Advanced Intermediate in the Lesion-Extrusion Pathway of hOGG1

  摘要：

  Here we present the first structure of a very advanced intermediate in the lesion-extrusion pathway of a DNA glycosylase, human 8-oxoguanine DNA glycosylase (hOGG1), and a substrate DNA containing a mutagenic lesion, 8-oxoguanine (oxoG). The structure was obtained by irradiation and flash-freezing of a disulfide-cross-linked (DXLed) complex of hOgg1 bound to DNA containing a novel photocaged derivative of oxoG. The X-ray structure reveals that upon irradiation, the oxoG lesion has transited from the exosite to the active site pocket, but has not undergone cleavage by the enzyme. Furthermore, all but one of the specificity-determining interactions between the lesion and the enzyme are unformed in the flashed complex (FC), because active site functionality and elements of the DNA backbone are mispositioned. This structure thus provides a first glimpse into the structure of a very late-stage intermediate in the lesion-extrusion pathway-the latest observed to date for any glycosylase-in which the oxoG has undergone insertion into the enzyme active site following photodeprotection, but the enzyme and DNA have not yet completed the slower process of adjusting to the presence of the lesion in the active site.

  DOI：

  10.1021/ja800821t

文献信息

• [EN] NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF<br/>[FR] COMPOSITIONS D'ACIDE NUCLÉIQUE-POLYPEPTIDE ET UTILISATIONS DE CELLES-CI
  申请人：AVIDITY BIOSCIENCES INC

  公开号：WO2020247782A1

  公开（公告）日：2020-12-10

  Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a cancer which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.

  本文披露了包括与修饰的多核苷酸分子和聚合物结合的结合基团的组合物和药物配方。本文还描述了利用包括结合基团与多核苷酸分子和聚合物结合的组合物或药物配方治疗癌症的方法。
• [EN] MODIFIED NUCLEOSIDE PHOSPHORAMIDITES<br/>[FR] PHOSPHORAMIDITES DE NUCLÉOSIDES MODIFIÉS
  申请人：ALIOS BIOPHARMA INC

  公开号：WO2019053659A1

  公开（公告）日：2019-03-21

  The present disclosure relates to compounds and compositions containing 5'-phosphoramidite nucleoside monomers of formulae (I) and (II), and methods of making and use, wherein the substituents are as defined in the appended claims.

  本发明公开涉及包含式(I)和式(II)的5'-磷酰胺基核苷单体的化合物和组合物，以及它们的制备和使用方法，其中取代基如所附权利要求中所定义。
• [EN] MULTIVALENT LIGAND CLUSTERS FOR TARGETED DELIVERY OF THERAPEUTIC AGENTS<br/>[FR] AGRÉGATS DE LIGANDS MULTIVALENTS POUR L'ADMINISTRATION CIBLÉE D'AGENTS THÉRAPEUTIQUES
  申请人：MITOTHERAPEUTIX LLC

  公开号：WO2020191183A1

  公开（公告）日：2020-09-24

  Targeting ligand clusters, and methods of preparing same, are described. A targeting ligand cluster may include first linkers attached to phenolic hydroxyl groups of gallic acid, and one or more targeting ligands attached to each of the first linkers. The targeting ligand cluster may also include a second linker attached to a carboxylic acid of the gallic acid, and at least one of a protecting group, a phosphoramidite, or an oligonucleotide attached to the second linker.

  描述了针对配体团簇以及制备方法。一个针对配体团簇可能包括连接到没食子酸酚羟基的第一连接剂，以及连接到每个第一连接剂的一个或多个靶向配体。该针对配体团簇还可能包括连接到没食子酸羧基的第二连接剂，以及至少一种保护基团、磷酰胺酯或寡核苷酸连接到第二连接剂。
• [EN] UNA AMIDITES AND USES THEREOF<br/>[FR] AMIDITES D'UNA ET LEURS UTILISATIONS
  申请人：AVIDITY BIOSCIENCES INC

  公开号：WO2020247818A1

  公开（公告）日：2020-12-10

  Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a disease which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.

  本文披露了包含结合基团与修饰的多核苷酸分子和聚合物结合的组合物和药物配方。本文还描述了利用包含结合基团与多核苷酸分子和聚合物结合的组合物或药物配方进行治疗疾病的方法。
• [EN] 4'-PHOSPHATE ANALOGS AND OLIGONUCLEOTIDES COMPRISING THE SAME<br/>[FR] ANALOGUES DE 4'-PHOSPHATE ET OLIGONUCLÉOTIDES COMPRENANT CEUX-CI
  申请人：DICERNA PHARMACEUTICALS INC

  公开号：WO2018045317A1

  公开（公告）日：2018-03-08

  Disclosed herein are oligonucleotides, such as nucleic acid inhibitor molecules, having a 4'-phosphate analog and methods of using the same, for example, to modulate the expression of a target gene in a cell. The phosphate analogs are bound to the 4'-carbon of the sugar moiety (e.g., a ribose or deoxyribose or analog thereof) of the 5'-terminal nucleotide of an oligonucleotide. Typically, the phosphate analog is an oxymethylphosphonate, where the oxygen atom of the oxymethyl group is bound to the 4'-carbon of the sugar moiety or analog thereof.

  本文披露了寡核苷酸，例如具有4'-磷酸盐类似物的核酸抑制分子，以及使用这些分子的方法，例如用于调节细胞中靶基因的表达。磷酸盐类似物与寡核苷酸的5'-端核苷酸的糖基（例如核糖或脱氧核糖或其类似物）的4'-碳结合。通常，磷酸盐类似物是氧甲基膦酸盐，其中氧甲基基团的氧原子与糖基或其类似物的4'-碳结合。