Process of preparation of olanzapine Form I
First Claim
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1. A process for preparing polymorphic olanzapine Form I comprising:
- a) reacting 4-amino-2-methyl-10H-thieno[2,3-b][1,5]benzodiazpine HCl and 1-methylpiperazine in an aprotic high boiling solvent or mixtures thereof at a temperature of between about 90°
C. to 130°
C.;
b) purifying the product of step a) in an acidic medium;
c) basifying the product of step b) to a pH of between 7.5-9; and
d) extracting the product of step c) using a low boiling organic solvent.
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Abstract
A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.
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Citations
22 Claims
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1. A process for preparing polymorphic olanzapine Form I comprising:
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a) reacting 4-amino-2-methyl-10H-thieno[2,3-b][1,5]benzodiazpine HCl and 1-methylpiperazine in an aprotic high boiling solvent or mixtures thereof at a temperature of between about 90°
C. to 130°
C.;
b) purifying the product of step a) in an acidic medium;
c) basifying the product of step b) to a pH of between 7.5-9; and
d) extracting the product of step c) using a low boiling organic solvent. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 22)
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17. A method for preparing olanzapine Form I comprising mixing 4-amino-2-methyl-10H-thieno[2,3-b][1,5]benzodiazepine hydrochloride with a mixture of 1-methylpiperazine, dimethylsulfoxide, toluene, and methanolic sodium hydroxide.
- 18. Olanzapine Form I having a polymorphic purity of at least 98%.
Specification