Synthesis of 2-Methyl-4-(4-Methyl-1-Piperazinly)-10H-Thieno(2,3-B) (1,5) Benzodiazepine and Salts Thereof
First Claim
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1. A process for the purification of olanzapine characterized in that said process comprises the following steps:
- a) mixing olanzapine with an organic acid in an organic solvent or a mixture of organic solvents to form an olanzapine acid addition salt,b) precipitating and isolating the olanzopine acid addition salt and,c) transformation of the olanzapine acid addition salt to olanzapine.
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Abstract
The invention belongs to the field of organic chemistry and relates to a new process for the purification of olanzapine comprising preparation of acid addition salts of olanzapine and transformation thereof into a pharmaceutically acceptable pure and discoloured final product. The present invention also relates to new processes for the preparation of pure olanzapine.
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Citations
37 Claims
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1. A process for the purification of olanzapine characterized in that said process comprises the following steps:
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a) mixing olanzapine with an organic acid in an organic solvent or a mixture of organic solvents to form an olanzapine acid addition salt, b) precipitating and isolating the olanzopine acid addition salt and, c) transformation of the olanzapine acid addition salt to olanzapine. - View Dependent Claims (2, 3, 4, 5, 6, 7, 35, 36)
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8-21. -21. (canceled)
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22. A process for the preparation of olanzapine in the form of an acid addition salt characterized in that said process comprises the following steps:
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a) 4-amino-2-methyl-10H-thieno[2,3-b][1,5]benzodiazepine hydrochloride is reacted with N-methylpiperazine to yield olanzapine and b) the obtained olanzapine is transformed to an acid addition salt thereof. - View Dependent Claims (23)
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24. A process for the preparation of olanzapine in the form of an acid addition salt characterized in that said process comprises the following steps:
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a) N-desmethylolanzapine is reacted with a methylating agent to yield olanzapine, b) the obtained reaction mixture is diluted with water and acidified with an acid, c) to the reaction mixture, an organic solvent is added and the phases are separated, d) the obtained water phase is neutralized and olanzapine is extracted with an organic solvent to obtain the organic solvent phase and e) an organic acid or substituted organic acid or an organic acid derivative of formula RX;
wherein R represents an organic radical such as acetyl, propionyl, chloroacetyl and X is selected from a group of Cl, Br or I;
or an organic acid anhydride;
is added to the organic phase to form a N substituted N-desmethylolanzopine derivative of formula 2 - View Dependent Claims (25, 26, 27)
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28-34. -34. (canceled)
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37-43. -43. (canceled)
Specification