| 摘要 |
Production of polymeric compounds (I) containing nucleo-base substituents comprises reacting compounds (II), (III), (IV) and (V) with one another, optionally simultaneously, and optionally removing one or more protecting groups and repeating the reaction m-times, with the product of the immediately preceding step being used in any subsequent step in place of (II). A = a residue of an amine component which is conventional in the Ugi reaction, e.g. H; a substituent; (cyclo)alkyl; (cyclo)alkenyl); (cyclo)alkynyl; (hetero)aroyl; heterocyclyl; or a fluorescence label, intercalator, antibiotic, minor or major groove binder, biotinyl group, intercalating agent, alkylating group, steroid, lipid, polyamine, agent facilitating cell reception, (oligo)saccharide, antisense polymer, peptide, antibody conjugate, synthetic polymer or corresponding modified surface; B = H a group or molecule specified under A; or a group X--NPG of compound (V); R1-G is a grouping of formula (i)-(iv): and is optionally bonded to (IV) through R, R1 or R4 via a molecular spacer; R and R1 = A or a residue of a natural or synthetic nucleo-base (at least one of R and R1 is such a residue); L, M, T and Z = O; S or NR4; R4 = H; F; (cyclo)alkyl; (cyclo(alkenyl); (cyclo)alkynyl; (hetero)aroyl; a heterocyclyl; -O-(cyclo)alkyl; -O-aroyl; -S-(cyclo)alkyl; or -S-aroyl; R2 and R3 = A, a residue of an oxo component which is conventional in the Ugi reaction, e.g. a group or molecule specified under A or a branching site P which is the starting site for a further DNA, RNA, PNA or peptide strand or another oligomer or polymer; X is a group of formula (v): PG = optionally orthogonal protecting groups, e.g. acyl, sulphonyl, alkyl or silyl or a carbamate or one of its salts; R5 = H; optionally substituted (cyclo)alkyl, alkoxyalkyl or aryl; or heterocyclyl; U, W, K and Y = optionally substituted (cyclo)alkyl, alkenyl, alkynyl, alkanoyl, alkoxyalkanoyl, aroyl or heterocyclyl; or NR5; a, b, c, n, o and p = 0-10, preferably 0-5; Q = optionally substituted (cyclo)alkyl, aryl, alkenyl, alkynyl, alkanoyl, alkoxyalkanoyl, cycloalkanoyl, aroyl or heterocyclyl; NR5; P; P(O); P(S); B; BR5; or SO2; F = O; S; Se or NH; J is a group of formula (vi)-(ix): R6 = H; a substituent; (cyclo)alkyl; (cyclo)alkenyl; (cyclo)alkynyl; (hetero)aroyl; or heterocyclyl.
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