Patent ID: 6762281
Filing Date: 2004-07-13
Classification: A61K,C07K

Abstract:
A method for preparing a peptide linked oligomeric compound comprising the steps of:(a) providing a support medium derivatized with a compound wherein said compound comprises a protected hydroxyl group; (b) treating said protected hydroxyl group with a deprotecting reagent effective to deprotect said hydroxyl group; (c) reacting said deprotected hydroxyl group with a 2â€²-, 3â€²-, or 5â€²-H-phosphonate nucleoside having a protected hydroxyl group and an activated phosphorus containing substituent group thereby forming an extended compound; (d) optionally treating said extended compound with a capping agent to form a capped compound; (e) optionally repeating steps (b), (c) and (d) to form a further extended compound; (f) treating said capped compound or said further extended compound with an oxidizing reagent thereby forming an oxidized compound comprising one or more nucleosides; (g) repeating steps (b), (c), (d), (e) and (f) for oxidized compounds comprising one nucleoside or optionally repeating steps (b), (c), (d), (e) and (f) for oxidized compounds comprising more than one nucleoside to give a further oxidized compound; (h) cleaving said oxidized compound or said further oxidized compound from the support medium to give said oligomeric compound comprising a linking moiety; (i) treating said linking moiety attached to said oligomeric compound with reagents effective to form a reactive sulfur moiety on said linking moiety; and (j) reacting said reactive sulfur moiety with a peptide wherein said peptide is functionalized with a functional group reactive with said sulfur moiety thereby forming said peptide linked oligomeric compound. 2.K The method of claim 1 wherein one of said reactive sulfur moiety and said functional group is â€”SH and the other of said reactive sulfur moiety and said functional group is a disulfide group.