The synthesis of the octadeoxyribonucleoside heptaphosphorothioate,
d[Tp(s)Tp(s)Gp(s)Gp(s)Gp(s)Gp(s)Tp(s)Vby the phosphouiester approach in solution is described. The phosphorothioate internucleotide linkages are protected by the S-(2-cyanoethyl) group and 1 -(mesitylene-2-sulfonyl)-3-nitro-1,2,4-lhl-triazole (MSNT) is used as the coupling agent. A block synthesis strategy (2 + 2 + 4 and 4 + 4 + 8) is followed.
INTRODUCTIONIn the past few years, there has been considerable interest in the large scale synthesis of phosphorothioate analogues1.2 of oligodeoxyribonucleides. A number of specific sequences have shown promise as chemotherapeutic agents, and several are at present undergoing clinical uiald. It appears from the literature that the consequent need for relatively large (certainly of the order of hundreds of grams and @ssibly considerably more) quantities of specific oligodeoxyribonucleotide phosphorothioates has almost
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