PREPARATION OF 5,8,13,14-TETRAHYDROBENZ(5,6)ISOINDOLO (2,1-B)ISOQUINOLIN-8,13-DIONE DERIVATIVES

摘要

A process is described for the preparation of compounds of formula (1) [where OR is hydroxyl, protected hydroxyl or OP(O)(OCH2Ph)(OR<1>) (where Ph is phenyl and OR<1> is hydroxyl or protected hydroxyl)] and salts thereof, which comprises reacting a compound of formula (2) with a compound of formula (3) (where OR is as defined above and one of X<1> and X<2> is a leaving group and the other is a hydrogen atom) or a salt thereof, followed, if desired, by removal of the hydroxyl protecting group when present and/or by salt formation. The compounds of formula (1) are either anticancer agents or intermediates useful in the synthesis of anticancer agents.