Process for the preparation of olanzapine

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C540S557000

Reexamination Certificate

active

07981884

ABSTRACT:
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.

REFERENCES:
patent: 5703232 (1997-12-01), Bunnell et al.
patent: 2004/0048854 (2004-03-01), Patel et al.
patent: 2005/0159408 (2005-07-01), Dolitzky et al.

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