主权项 |
1. A bicyclic nucleoside analog of Formula Ie:wherein:
Bx is a heterocyclic base moiety; Q is a bridge group comprising one C(R3)═C(R4), N(R5)—O or N(R5)—S biradical group and one C(R3)(R4) biradical group or one O, S or N(R5) biradical group and two C(R3)(R4) biradical groups; each R3 and R4 is, independently, H, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkoxy, substituted C1-C6 alkoxy or halogen; R5 is H, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkoxy or substituted C1-C6 alkoxy; L1 and L2 are each H or one of L1 and L2 is H and the other of L1 and L2 is CH3 or OCH3; one of E1, E2, E3 and E4 is O-T2, two of E1, E2, E3 and E4 are H and the remaining one of E1, E2, E3 and E4 is H, halogen, C1-C6 alkyl or substituted C1-C6 alkyl; one of T1 and T2 is H, a hydroxyl protecting group or a phosphorus moiety and the other of T1 and T2 is H, a hydroxyl protecting group or a reactive phosphorus group. each substituted group comprises one or more optionally protected substituent groups independently selected from halogen, OJ5, N(J5)(J6), =NJ5, SJ5, N3, CN, OC(=L)J5, OC(=L)N(J5)(J6) and C(=L)N(J5)(J6); L is O, S or NJ7; and each J5, J6 and J7 is, independently, H, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C5-C20 aryl or C1-C12 aminoalkyl. |