A process for producing pure form of...

Details A process for producing pure form of... A process for producing pure form of...

C - Chemistry, Metallurgy

07

D

C07D 243/10 (2006.01)

Patent

CA 2576862

Disclosed is a process for producing pure form of 2-methyl-4-(4-methyl-1- piperazinyl)-10H-~thieno[2,3-b][1,5] benzodiazepine. The process comprises of reacting 2-(2-aminoanilino)-5-~methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2- methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4- methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine in a mixture of solvents.

La présente invention concerne un procédé permettant de produire une forme pure de 2-methyl-4-(4-methyl-1-piperazinyl)-10H--thieno[2,3-b][1,5] benzodiazepine. Le procédé décrit dans cette invention consiste à faire réagir 2-(2-aminoanilino)-5--methylthiophene-3-carbonitrile avec N-methyl piperazine conjointement avec un sel acide de N-methylpiperazine, pour produire du 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine. La présente invention concerne également un procédé permettant d'obtenir une forme polymorphe de 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine par cristallisation de 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine brut dans un mélanges de solvants.

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