Methods for preparation of olanzapine polymorphic form i
AssigneeInstitut Farmaceutyczny
InventorsJanina Piechaczek, Magdalena Glice, Urszala Fraczek, Jadwiga Serafin, Wieslaw Szelejewski, Krzysztof Soltysiak
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Abstract
The invention relates to the methods for preparation of olanzapine polymorphic Form I. The invention also provides new mixed solvates of olanzapine, which are valuable intermediates used in the preparation of pure olanzapine polymorphic Form I.
Claims13
Method for preparation of pure olanzapine polymorphic Form I, characterized in that the crude olanzapine prepared by condensation of molar excess of N-methylpiperazine with 4-amine-2-methyl-10H-thieno[2,3-b][1,5]benzodiazepine hydrochloride carried out in dimethylsulfoxide, is recovered from the reaction mixture and purified by using methylene chloride as the same, single solvent.
Solvate (1) of crude olanzapine with CH2Cl2 and water in proportion 4 molecules of olanzapine:
- 1 molecule of CH2Cl2:
- 8 molecules of water.
Solvate (2) of crude olanzapine with dimethylsulfoxide and water in proportion of 4 molecules of olanzapine:
- 1 molecule of DMSO:
- 2 molecules of water.
Solvate (2) characterized by bands in a IR spectrum recorded from KBr pellet at the following wavenumbers (cm−1):
- 3358, 3233, 2922, 2848, 1591, 1467, 1412, 1366, 1282, 1263, 1219, 1149, 1004, 970, 851, 754.
Dependencies are inferred from the claim text.