Patent ID: 6124450
Filing Date: 2000-09-26
Classification: A61P,C07F,C07H

Abstract:
A synthetic process comprising contacting a compound having formula I with a coupling reagent having formula [(R.sub.N).sub.2 N].sub.2 PO(CH.sub.2).sub.x Si(R.sub.S).sub.3 for a time and under reaction conditions effective to form a compound having formula II: ##STR9## wherein: each Q is, independently, O, S, CH.sub.2, CHF or CF.sub.2 ;each B.sub.x is, independently, a nucleosidic base;each X is, independently, H, OH, alkyl, substituted alkyl, alkaryl or aralkyl, F, Cl, Br, CN, CF.sub.3, OCF.sub.3, OCN, O-alkyl, S-alkyl, N-alkyl, O-alkenyl, S-alkenyl, N-alkenyl, SOCH.sub.3, SO.sub.2 CH.sub.3, ONO.sub.2, NO.sub.2, N.sub.3, NH.sub.2, heterocycloalkyl, heterocycloalkaryl, aminoalkylamino, polyalkylamino or substituted silyl;R.sub.HP is a hydroxyl protecting group;each R.sub.N is, independently, alkyl having 1 to about 10 carbon atoms;each R.sub.S is, independently, alkyl having 1 to about 10 carbon atoms or aryl having 6 to about 10 carbon atoms; andx is 1 to about 7.