PROCESS FOR PREPARING 6-BETA-(3-AMINOSUBSTITUTED PROPIONYLOXY) FORSCOLINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF Russian patent published in 1995 - IPC

FIELD: in medicine for the treatment of cardiovascular diseases. SUBSTANCE: Reagent 1: forscoline, Reagent 2: acetone. Reaction conditions: in the presence of HCl. Reagent 3: a 1,9-isopropylidene derivative of forscoline. Reagent 4: alkali in alcohol. Reagent 5: a 7-diacetyl derivative or 1,9-isopropylidene derivative of forscoline. Reagent 6: beta-halopropionylhedine. Reaction conditions: in the presence of an organic base treatment of the resulting compound with alkali and deprotection at the 1,9-position of the resulting (3-substituted amino)propionyloxy derivative of forscoline and isolation of the desised product in the free state or as a pharmaceutically acceptable salt and optionally conversion into a 7-acetoxyderivative. The stage of reaction with an amine as well as a stage of reaction with an amine and a deprolection stage may be carried out in any sequence. The first and second stages as well as the fifth and sixth stages may be accomplished in a single stage. EFFECT: more efficient preparation process. 2 cl