A method for converting 9-deoxyforskolin of formula (II) to forskolin of formula (I) comprises (i) hydrolysis of (II), (ii) reacting the prod. with 1,1'-carbonylidiimidazole or 2,2dimethoxypropane, (iii) reacting the cpd. obtd. with dimethyl sulphate and potassium hydride, (iv) reacting the prod. with a peroxy acid, (v) acid hydrolysis, (vi) hydrolysis and (vii) acetylation of the hydroxy gp. at position 7 to obtain (I). Cpd. (I) is used as an intermediate for the regioselective and stereoselective synthesis of forskolin from 9- deoxyforskolin in a good yield.
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