Process for the preparation of nucleoside derivatives

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) C07H 19/04 (2006.01)

Patent

CA 2119914

2119914 9307162 PCTABS00021 The invention concerns a process for the preparation of nucleoside derivatives espcecially of AZT. As the starting material a 2,3'-anhydroderivative of the said nucleoside is used, which in its 5'-position carries a largish protecting group, which is stable under weakly alkaline, but which is split off in strongly alkaline conditions, especially pivaloyl, or adamantoyl. This compound is reacted with sodium or potassium azide and lithium halide in the presence of a buffering salt, whereafter the 5'-protecting group is split off from the obtained 3'-azido-nucleoside by treating with a base.

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