PROCESS FOR PRODUCING ACYLATED ETOPOSIDE DERIVATIVES AND PHARMACEUTICAL PREPARATIVES CONTAINING SUCH ACTIVE SUBSTANCE

摘要

The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia wherein R<2> is H and R<1> is selected from the group consisting of (C1-10)alkyl, (C2-10)alkenyl, (C5-6)cycloalkyl, 2-furyl, 2-thienyl, (C6-10)aryl, and (C7-14)aralkyl; or R<1> and R<2> are each (C1-10)alkyl; or R<1>, R<2> and the carbon to which they are attached together represent (C5-6)cycloalkyl; one of R<3> and R<4> is H and the other is selected from the group consisting of (C1-5)alkanoyl and benzoyl; or R<3> and R<4> are the same or different and are selected from the group consisting of (C1-5)alkanoyl and benzoyl; R<5> is H or a phosphate group.