Process for preparing ziprasidone

Details Process for preparing ziprasidone Process for preparing ziprasidone

C - Chemistry, Metallurgy

07

D

C07D 417/12 (2006.01) A61K 31/428 (2006.01) A61P 25/18 (2006.01)

Patent

CA 2581322

The present invention concerns a process for the preparation of 5-(2-(4-(1,2- 5 benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2- one of the formula (I), or a pharmaceutically acceptable acid addition salt, solvate, hydrates or clathrate thereof, said process comprising reacting a compound of formula (II) wherein X is a halogen atom, with a compound of formula (III), said compound of formula (III) being the free base or an addition salt with an organic or inorganic acid, wherein said process is characterized in that said compounds according to formulas (II) and (III) are reacted in the presence of a neutralizing agent, and are reacted in a solvent comprising acetonitrile.

L'invention concerne un procédé de préparation d'une 5-(2-(4-(1,2-5 benzisothiazol-3-yl)-1-pipérazinyl)éthyl)-6-chloro-1,3-dihydro-2H-indol-2-one de la formule (I), ou d'un sel d'addition acide, d'un solvate, d'hydrates ou d'un clathrate pharmaceutiquement acceptables de cette dernière, lequel procédé consiste à faire réagir un composé de la formule (II), dans laquelle X est un atome d'halogène, avec un composé de la formule (III), ledit composé de la formule (III) étant la base libre ou un sel d'addition avec un acide organique ou inorganique, le procédé de l'invention étant caractérisé en ce que les composés des formules (II) et (III) sont mis à réagir en présence d'un agent neutralisant, et sont mis à réagir dans un solvant comprenant de l'acétonitrile.

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