Santaris Pharma A/s

Mads Detlef Sørensen

Troels Koch

Christoph Rosenbohm

Jesper Wengel

Daniel Sejer Pedersen

Signe M Christensen

Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.

Synthesis of locked nucleic acid derivatives

The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as &#x3b1;--oxy-LNA, amino-LNA, &#x3b1;--amino-LNA, thio-LNA, &#x3b1;--thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilizing intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. 

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København N, Denmark

Mads Detlef Sørensen