[EN] PREPARATION OF INTERMEDIATES USEFUL IN THE SYNTHEIS OF 2'-CYANO-2'-DEOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE<br/>[FR] PRÉPARATION D'INTERMÉDIAIRES UTILES DANS LA SYNTHÈSE DE 2'-CYANO-2'-DÉSOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE
申请人:CYCLACEL LTD
公开号:WO2009136158A1
公开(公告)日:2009-11-12
The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2'; (ii) converting said compound of formula 682-2' into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4 -palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
本发明涉及一种制备式682-4化合物的方法,该方法包括以下步骤:(i)将式682-1化合物转化为式682-2'化合物;(ii)将所述式682-2'化合物转化为式682-3化合物;以及(iii)将所述式682-3化合物转化为式682-4化合物。该发明的进一步方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-β-D-阿拉伯莫呋核苷的用途,这是一种嘧啶核苷,对治疗和/或预防癌症具有治疗作用。