Process for the preparation of high purity buspiron and the hydrochloride thereof

摘要

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 continuously adding a solution of 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) formed with an inert organic solvent having a concentration of at least 40% by weight to a suspension of a hydrogenation 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.