C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/14 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2128164
A b s t r a c t The invention relates to a process for the preparation of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]- -8-aza-spiro[4,5]decane-7,9-dione (buspiron) of the Formula I Image (I) and the hydrochlorides thereof having high purity by subjecting 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]- -but-2-inyl]-8-aza-spiro[4,5]decane-7,9-dione of the Formula II Image (II) to catalytic hydrogenation in the presence of a palladium or Raney-nickel catalyst in an inert organic solvent and optionally converting the 8-[4-[4-(pyrimidine-2-yl)- -piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione thus obtained into the hydrochloride thereof which comprises continuously adding a solution 8-[4-[4- -(pyrimidine-2-yl)-piperazine-1-yl]-but-2-inyl]-8-aza- -spiro[4.5]decane-7,9-dione formed with an inert organic solvent having a concentration of at least 40 % by weight to a suspension of a catalyst in an inert organic solvent, removing the catalyst and subsequently a) isolating the 8-[4-[4-(pyrimidine-2-yl)-piperazine- -1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione base and/or b) treating the 8-[4-[-(pyrimidine-2-yl)-piperazine-1- -yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione base with hydrogen chloride in ethanol or isopropanol under stirring at a temperature between 15 °C and 40 °C and isolating the 8-[4-[4-(pyrimidine-2-yl)- -piperazine-1-yl]-butyl]-8-aza-spiro [4.5]decane-7,9- -dione hydrochloride melting at 188-191 °C, or c) treating the 8-[4-[4-(pyrimidine-2-yl)-piperazine-1- -yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione base with hydrogen chloride in ethyl acetate or isopro- panol at a temperature not exceeding 70°C under stirring and isolating the 8-[4-[4-(pyrimidine-2-yl)- -piperazine-1-yl]-butyl]-8-aza-spiro [4.5]decane-7,9- -dione hydrochloride melting at 201-203 °C.
Blasko Gabor
Budai Zoltan
Csorgo Margit
Furdyga Eva
Klebovich Imre
Egis Gyogyszergyar Rt.
Fetherstonhaugh & Co.
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