bis(diisopropylamino)(2-cyanoethoxy)phosphane | 133485-25-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: bis(diisopropylamino)(2-cyanoethoxy)phosphane
• 英文别名: 2-cyanoethyl bis(N,N-diisopropyl)phosphorodiamidite；2-cyanoethyl-bis-(N,N-diisopropyl)-phosphoramidite；2-cyanoethyl-N,N-diisopropylphosphoramidite；2-cyanoethyl N,N-diisopropylhydroxyphosphoramidite；cyanoethyl N,N-diisopropylphosphoramidite；N,N-diisopropyl-O-β-cyanoethyl phosphoramidite；N,N-diisopropyl-cyanoethyl phosphoramiditechloride；2-cyanoethoxy-N,N-diisopropyl phosphoramidite；2-cyanoethyl diisopropylchlorophosphoramidite；N,N-diisopropyl-O-cyanoethyl phosphoramidite；2-cyanoethyl-N,N-diisopropylaminochlorophosphoramidite；β-cyanoethyl-N,N-diisopropyl phosphoramidite；N,N-diisopropyl-beta-cyanoethylphosphoramidite；2-cyanoethyl-N,N-diisopropylphosphoroamidite；2-cyanoethoxy-N,N-di(propan-2-yl)phosphonamidous acid
• CAS: 133485-25-3
• 化学式: C₉H₁₉N₂O₂P
• 分子量: 218.236
• InChiKey: FINYOTLDIHYWPR-UHFFFAOYSA-N

物化性质

• 沸点：
  324.1±44.0 °C(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  56.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  bis(diisopropylamino)(2-cyanoethoxy)phosphane 在 2,6-二甲基吡啶 、 三氯化磷 作用下， 以 四氢呋喃 为溶剂， 反应 2.58h， 生成 C₉H₁₈Cl₂N₂O₂P₂
  参考文献：
  名称：

  从固相环水杨基磷酸化试剂合成核苷单、二和三磷酰胺

  摘要：

  在碳酸钾的存在下，氯甲基聚苯乙烯树脂与 5-羟基水杨醛反应，得到聚合物结合的 2-羟基苯甲醛。随后用硼烷溶液还原产生聚合物结合的 2-羟基苯甲醇。固定化的 2-羟基苯甲醇与适当的亚磷酸酯化试剂反应生成固相环水杨基单-、二-和三亚磷酸酯化试剂，其与未保护的核苷反应，随后碘氧化、氰乙氧基脱保护和碱性裂解，分别以52-73% 的总产率提供 5'- O-核苷单-、二-和三氨基磷酸酯。

  DOI：

  10.1021/ol900320r
• 作为产物：
  描述：

  二异丙胺 在 水 作用下， 以 乙腈 为溶剂， 反应 0.67h， 生成 bis(diisopropylamino)(2-cyanoethoxy)phosphane
  参考文献：
  名称：

  Selective Diphosphorylation, Dithiodiphosphorylation, Triphosphorylation, and Trithiotriphosphorylation of Unprotected Carbohydrates and Nucleosides

  摘要：

  [GRAPHIC]Aminomethyl polystyrene resin-bound linkers of p-acetoxybenzyl alcohol were subjected to reactions with diphosphitylarting and triphosphitylating reagents to yield the corresponding polymer-bound cliphosphitylating and triphosphitylating reagents, respectively. A number of unprotected carbohydrates and nucleosides were reacted with the polymer-bound reagents. Oxidation with tert-butyl hydroperoxide or sulfurization with Beaucage's reagent, followed by removal of cyanoethoxy group with DBU and the acidic cleavage, respectively, afforded only one type of monosubstituted nucleoside and carbohydrate diphosphates, dithiodi phosphates, triphosphates, and trithiotriphosphates with high regioselectivity.

  DOI：

  10.1021/ol0521432

文献信息

• [EN] CYCLIC DINUCLEOTIDES AS AGONISTS OF STIMULATOR OF INTERFERON GENE DEPENDENT SIGNALLING<br/>[FR] DINUCLÉOTIDES CYCLIQUES UTILISÉS EN TANT QU'AGONISTES DU STIMULATEUR DE LA SIGNALISATION DÉPENDANTE DU GÈNE DE L'INTERFÉRON
  申请人：UNIV TEXAS

  公开号：WO2018156625A1

  公开（公告）日：2018-08-30

  Disclosed herein are new cyclic dinucleotide compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulation of immune response to disease, and induce Stimulator of Interferon Genes (STING) dependent type I interferon production and co-regulated genes in a human or animal subject are also provided for the treatment diseases such as cancer, particularly metastatic solid tumors and lymphomas, inflammation, allergic and autoimmune disease, infectious disease, and for use as anti-viral agents and vaccine adjuvants.

  本文披露了新的环二核苷酸化合物和组合物，以及它们作为药物治疗疾病的应用。还提供了调节免疫应答以及诱导干扰素基因激活剂（STING）依赖型I干扰素在人类或动物受试者中产生和共调控基因的方法，用于治疗癌症、尤其是转移性实体瘤和淋巴瘤、炎症、过敏和自身免疫疾病、传染病，以及作为抗病毒剂和疫苗佐剂的用途。
• SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES
  申请人：AM Chemicals LLC

  公开号：US20180016232A1

  公开（公告）日：2018-01-18

  Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.

  揭示了用于制备含有至少一个非核苷酸基团与实用兴趣配体共轭的合成寡核苷酸的新型非核苷酸固相支持体和磷酰胺酸酯构建块，以及制备这些固相支持体和磷酰胺酸酯构建块的合成过程。此外，使用所述固相支持体和磷酰胺酸酯构建块制备寡聚合物化合物，最好是在去除保护基的情况下，以提供与感兴趣的配体共轭的寡核苷酸。
• [EN] NUCLEOSIDE-LIPID COMPOUNDS WITH PH-SENSITIVE DIALKYLORTHOESTER CHAINS AND THEIR USE FOR TRANSPORTATION OR VECTORIZATION OF AT LEAST ONE THERAPEUTIC AGENT<br/>[FR] COMPOSÉS NUCLÉOSIDES-LIPIDES AVEC DES CHAÎNES DIALKYLORTHOESTER SENSIBLES AU PH ET LEUR UTILISATION POUR LE TRANSPORT OU LA VECTORISATION D'AU MOINS UN AGENT THÉRAPEUTIQUE
  申请人：UNIV BORDEAUX

  公开号：WO2016188868A1

  公开（公告）日：2016-12-01

  The invention relates to new nucleoside-lipid compounds with pH-sensitive dialkylorthoesterchains, to the process for their preparation and to their uses, in particular their use for transportation or vectorization of at least one therapeutic agent.

  这项发明涉及具有pH敏感二烷基正酯链的新核苷脂类化合物，涉及它们的制备过程以及它们的用途，特别是用于运输或载体化至少一种治疗剂的用途。
• NOVEL STING AGONISTS
  申请人：Venenum Biodesign, LLC

  公开号：US20200131209A1

  公开（公告）日：2020-04-30

  The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

  本发明提供了式I′的化合物： 其中 , W, X, Y, Z, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 和R 5 如本文所定义，或其立体异构体、互变异构体、药学上可接受的盐、前药酯或溶剂化合物形式，其中所有变量均如本文所定义。这些化合物能有效调节STING蛋白，因此可用作治疗或预防受STING激动影响的疾病的药物。
• Nucleic Acid Probes, their Synthesis and Use
  申请人：Atlas Genetics Limited

  公开号：US20160025703A1

  公开（公告）日：2016-01-28

  The invention provides a method of probing for a nucleic acid comprising: contacting a nucleic acid solution with an oligonucleotide probe labelled with an electrochemically active marker, providing conditions at which the probe is able to at least partially hybridise with any complementary target sequence which may be present in the nucleic acid solution, selectively degrading either hybridised, partially hybridised or unhybridised nucleic acid probe, and electrochemically determining information relating to the electrochemically active marker. The invention further provides novel molecules with use in methods of the invention.

  这项发明提供了一种探测核酸的方法，包括：将核酸溶液与标记有电化学活性标记物的寡核苷酸探针接触，在探针能够至少部分与核酸溶液中可能存在的任何互补靶序列杂交的条件下提供条件，选择性地降解已杂交、部分杂交或未杂交的核酸探针，并电化学地确定与电化学活性标记物相关的信息。该发明还提供了在该方法中使用的新型分子。