The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (O-[(2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl}O,O-dihydrogen phosphorothioate, also known as 2'-(S)-fluoro-thio-adenosine monophosphate or 2'-F-thio-AMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
本发明涉及有效的过程,用于制备
氟代核苷,例如(O-[(2R,3R,4S,5R)-5-(6-
氨基-9H-
嘌呤-9-基)-4-
氟-3-羟基氧杂
环己烷-2-基]甲基}O,O-二氢
磷酸硫酯,也称为2'-(S)-
氟硫腺苷酸单
磷酸酯或2'-F-
硫-
AMP。这种
氟代核苷可以用作
生物活性化合物,或用作更复杂
生物活性化合物的合成中间体。本发明还涵盖了在所披露的合成过程中有用的中间体及其制备方法。