PROCESS FOR THE PREPARTION OF OLANZAPINE

The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organ...

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Hauptverfasser: NEMETH GABOR, KOVANYINE LAX GYORGYI, NAGY KALMAN, KRASZNAY GYORGY, MESTERHAZY NORBERT, VERECZKEYNE DONATH GYORGYI, SZENT-KIRALLYI ZSUZSANNA
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creator NEMETH GABOR
KOVANYINE LAX GYORGYI
NAGY KALMAN
KRASZNAY GYORGY
MESTERHAZY NORBERT
VERECZKEYNE DONATH GYORGYI
SZENT-KIRALLYI ZSUZSANNA
description The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1,3-dimethyl-2-imidazolidinone. The invention also encompasses new 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2,3-b][1,5]benzodiazepine dihydrochloride trihydrate of the formula (IB), the preparation thereof and pharmaceutical compositions comprising said new compound.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title PROCESS FOR THE PREPARTION OF OLANZAPINE
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