| 1357354-90-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• CAS: 1357354-90-5
• 化学式: C₂₂H₃₃N₁₀O₈P
• 分子量: 596.54
• InChiKey: NDSOMGOABWJXNA-PTFPVMSCSA-N

反应信息

• 作为产物：
  描述：

  、 [9-[(2R,6S)-6-[[chloro(dimethylamino)phosphoryl]oxymethyl]-4-tritylmorpholin-2-yl]-2-(2-methylpropanoylamino)purin-6-yl] N,N-diphenylcarbamate 在 N-乙基吗啉 、 lithium bromide 、 3-cyanopyridine trifluoroacetate 、 ammonium hydroxide 、 甲胺 作用下， 以 1,3-二甲基-2-咪唑啉酮 、 二氯甲烷 、 2,2,2-三氟乙醇 为溶剂， 反应 1.05h， 以46%的产率得到
  参考文献：
  名称：

  Development of an efficient method for phosphorodiamidate bond formation by using inorganic salts

  摘要：

  Phosphorodiamidate morpholino oligonucleotides (PMOs) have been extensively applied in antisense strategies for gene regulation because of their high stability in serum and low toxicity. However, chain elongation of PMOs requires long reaction time because few efficient methods have been developed for the formation of phosphorodiamidate bonds. In this Letter, we examined the effect of various additives to improve the reaction efficiency for formation of the phosphorodiamidate bond in the synthesis of PMOs. The addition of certain inorganic salts to the reaction media was found to be more effective. Particularly, lithium bromide was the most effective reagent and led to considerable acceleration (ca. 10-fold improvement). (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.12.021