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

Abstract：

: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).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Harakawa T,Tsunoda H,Ohkubo A,Seio K,Sekine M

doi

10.1016/j.bmcl.2011.12.021

subject

Has Abstract

pub_date

2012-02-01 00:00:00

pages

1445-7

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01693-3

journal_volume

22

pub_type

杂志文章

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