A PROCESS FOR PRODUCING PURE FORM OF 2-METHYL-4-(4-METHYL-1-PIPERAZINYL)-10H-THIENO[2,3-b][1,5]BENZODIAZEPINE

A PROCESS FOR PRODUCING PURE FORM OF 2-METHYL-4-(4-METHYL-1-PIPERAZINYL)-10H-THIENO[2,3-b][1,5]BENZODIAZEPINE

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...

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Hauptverfasser: BHATNAGAR, AKSHAT, THAPER, RAJESH, KUMAR, SHASTRI, JWALANT, ASHESH, DUBEY, SUSHIL, KUMAR
Format: Patent
Sprache:eng ; fre
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Zusammenfassung: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.