FORSKOLIN DERIVATIVES

摘要

This invention relates to forskolin derivatives, their physiologically acceptable salts having positive inotropic, hypotensive and adenylate cyclase-stimuling action, and a process for producing these compounds. The forskolin derivative is represented by the general formula <IMG> wherein; I. when R1 is hydrogen and R4 is vinyl, ethyl, or cyclopropl, (1) either of R2 and R3 deonotes a residue represented by the formula CO(CH2)m <IMG> ,wherein each of R5 and R6 denotes hydrogen or lower alkyl or R5 and R6 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 R2 and R3 denotes hydrogen or a residue represented by the formula CO(CH2)nX, X being hydrogen or <IMG> wherein, each of R7 and R8 denotes hydrogen or lower alkyl or R7 and R8 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) R2 denotes hydrogen or -COCH2CH2CO2H and R3 denotes hydrogen, -COCH3, -COCH2CH2CH2CO2H, or -COCH(OH)CH2OH with the proviso that R3 is one of the last two residues when R2 is hydrogen, and II. when R1 is a residue represented by the formula of CO(CH2)pCO2H and CO(CH2) <IMG> wherein, each of R9 and R10 denotes hydrogen or lower alkyl, p is an integer of 0 to 5, and q is an integer of 1 to 5, R2 denotes hydrogen, R3 denotes acetyl, and R4 denotes vinyl.