The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as &agr;-L-oxy-LNA, amino-LNA, &agr;-L-amino-LNA, thio-LNA, &agr;-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising 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.
1
该发明涉及一种用于合成锁定核酸衍
生物的新策略,例如α-L-氧基-LNA、
氨基-LNA、α-L-
氨基-LNA、
硫基-LNA、α-L-
硫基-LNA、
硒基-LNA和亚甲基-LNA,该策略利用中间体进行可扩展的高产率反应,这些中间体还可以产生其他LNA类似物,如氧基-LNA。另外,公式X的化合物是重要的中间体,可以与多种亲核试剂反应,生成各种LNA类似物。