| 摘要 |
<p>A pyrrolobenzodiazepine derivative has the formula (I) or formula (II) wherein: X is COOH, NHZ, SH, or OH; Z is H or an amine protecting group; A is O, S, NH, or a single bond; R2 and R3 are independently H, R, OH, OR, =O, =CH-R, =CH2, CH2-CO2R, CH2-CO2H, CH2-SO2R, O-SO2R, CO2R, COR or CN and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, and R9 are independently H, R, OH, OR, halo, nitro, amino or Me3Sn; R11 is H or R; Q is S, O or NH; R10 is a nitrogen protecting group; R is optionally substituted alkyl; alkyl-C(O)-alkyl; alkyl- O-alkyl; alkyl-S-; aralkyl or aryl group with the alkyl and the alkyl portion of the aralkyl group optionally containing one or more carbon-carbon double or triple bonds, which may form part of a conjugated system; Y is a divalent group such that HY=R X' is CO, NH, S or O; T is a combinatorial unit and n is a positive integer. The compounds of formula (I) or (II) can also be linked to a solid support and are useful in synthesizing other pyrrolobenzodiazepine derivatives.</p> |
