Enzyme catalyzed therapeutic agents

A compound of the formula:

• 56
• wherein:
• R1 is a moiety of the formula:
• 57
• R2 is a divalent electron conduit moiety selected from the group consisting of:
• an unsaturated hydrocarbyl group;
• an aromatic hydrocarbyl group comprising one or more unsaturated hydrocarbyl groups;
• and,
• a heteroaromatic group comprising one or more unsaturated hydrocarbyl groups;
• R3 is a divalent spacer moiety selected from the group consisting of:
• 58
• R5 may be the same or different and is independently a linear or branched alkyl group having from 1 to 10 carbon atoms, or a cycloalkyl group having from 3 to 10 carbon atoms;
• n is an integer from 0 to 10;
• m is 0 or 1;
• R4 is a toxophore moiety selected from the group consisting of:
• 59
• X is —Cl, —Br, —I, or other potent leaving group, with the proviso that when R7 is —H, and M is zero, then R4 is not a halogen or when m is zero and n is zero, then R4 is not a halogen;
• Y is independently —H or —F;
• Z is independently —O— or —S—;
• Q is a sugar moiety selected from the group consisting of:
• 60
• R6 is independently —H, —OH, —OC(═O)CH3, or other protected hydroxyl group;
• and,
• R7 is hydrogen, a phosphate group, or a phosphoramidate group;
• and wherein said compound may be in any enantiomeric, diasteriomeric, or stereoisomeric form, including, D-form, L-form, α-anomeric form, and β-anomeric form.

A method of forming a compound of the formula:

• 85
• wherein “Base” denotes a nucleic acid base;
• which method comprises the step of reacting a compound of the formula:
• 86
• with a compound of the formula:
• 87
• in the presence of an HCl scavenger.

A method of forming a compound of the formula:

• 88
• wherein R1 is a substituent;
• which method comprises the step of reacting a compound of the formula:
• 89
• with a compound of the formula:
• 90
• in the presence of an HCl scavenger.