期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 3, 页码 1445-1447出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.021
关键词
Morpholino nucleic acid; Phosphorodiamidate bond; Inorganic salt catalysis
资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan
- global COE, Ministry of Education, Culture, Sports, Science and Technology, Japan
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.
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