abstract |
This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these com D ounds. The forskolin derivative is represented by the general formulan wherein;n I. when R' is hydrogen and R 4 is vinyl, ethyl, or cyclopropyl,n (1) either of R 2 and R 3 denotes a residue represented by the formulan wherein each of R 5 and R 6 denotes hydrogen or lower alkyl or R 6 and R 6 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom and m is an integer of 1 to 5, and the other one of R 2 and R 3 denotes hydrogen or a residue represented by the formula CO(CH 2 ) n X, X being hydrogen orn wherein, each of R 7 and R 8 denotes hydrogen or lower alkyl or R 7 and R 8 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom, and n being an integer of 1 to 5, or (2) R 2 denotes hydrogen or -COCH 2 CH 2 CO 2 H and R 3 denotes hydrogen, -COCH 3 , -COCH 2 CH 2 CH 2 CO 2 H, or -COCH(OH)CH 2 OH with the proviso that R 3 is one of the last two residues when R 2 is hydrogen, and II. when R' is a residue represented by a formula of CO(CH 2 ) p CO 2 H andn wherein, each of R 9 and R 10 denotes hydrogen or lower alkyl, p is an integer of 0 to 5, and q is an integer of 1 to 5,n R 2 denotes hydrogen, R 3 denotes acetyl, and R 4 denotes vinyl. |