Patent ID: 6020475
Filing Date: 2000-02-01
Classification: C07H

Abstract:
A method for the preparation of an oligomeric compound having a moiety of Formula I: ##STR38## wherein: X.sub.4 is Z or H;Z is CN, halogen, alkaryl, substituted sulfoxyl, substituted sulfonyl, or a substituted thio group, wherein said substituent is alkyl, aryl, or alkaryl; andX.sub.1 is O or S;comprising the steps of:(a) providing a compound having the Formula II: ##STR39## wherein: each R.sub.1, is, independently, H, --OH, --F, or --O--X.sub.3 --D;X.sub.3 is alkylenyl having from 1 to 10 carbons;D is H, amino, protected amino, alkyl substituted amino, imidazolyl, or (--O--X.sub.3).sub.p H where p is 1 to about 10;each X.sub.2 is O or S;R.sub.3 is selected from the group consisting of hydrogen, a hydroxyl protecting group, and a linker connected to a solid support;each B, independently, is selected from the group consisting of a naturally occurring nucleobase, a non-naturally occurring nucleobase, a protected naturally occurring nucleobase, and a protected non-naturally occurring nucleobase;n is 0 to about 50;each Q is --X.sub.1 H or ##STR40## R.sub.5 is selected from the group consisting of --N(R.sub.6).sub.2, a heterocycloalkyl ring containing from 4 to 7 atoms, and having up to 3 heteroatoms selected from nitrogen, sulfur, and oxygen, and a heterocycloalkenyl ring containing from 4 to 7 atoms, and having up to 3 heteroatoms selected from nitrogen, sulfur, and oxygen; andR.sub.6 is straight or branched chain alkyl having from 1 to 10 carbons; and(b) reacting the compound of Formula II with a compound having Formula III: ##STR41## wherein R.sub.3a is hydrogen; and R.sub.2 is a hydroxyl protecting group, or a linker connected to a solid support, provided that R.sub.2 and R.sub.3 are not both simultaneously a linker connected to a solid support;to form the oligomeric compound.