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Details for Patent: 5,703,232

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Details for Patent: 5,703,232

Title: Process and solvate of 2-methyl-thieno-benzodiazepine
Abstract:The invention provides lower alcohol solvates of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine (olanzapine) and a process for making such lower alcohol solvates of olanzapine. The invention provides a method for using such solvates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.
Inventor(s): Bunnell; Charles A. (Lafayette, IN), Hotten; Terrence Michael (Farnborough, GB2), Larsen; Samuel D. (West Lafayette, IN), Tupper; David Edward (Reading, GB2)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Filing Date:Jan 16, 1996
Application Number:08/586,431
Claims:1. A process for preparing substantially pure Form I olanzapine comprising drying a C.sub.1 -C.sub.3 alcohol solvate of olanzapine, and then crystallizing the dried solvate with one or more solvents selected from ethyl acetate, acetone, 2-propanol, t-butanol, tetrahydrofuran and toluene.

2. A process of claim 1 wherein the solvate is contacted with the solvent at a temperature from about 25.degree. C. to 80.degree. C.

3. A process of claim 2 wherein the solvent is ethyl acetate.

4. A process of claim 3 wherein the solvate is a mono(methanol) solvate.

5. A process of claim 3 wherein the solvate is a mono(ethanol) solvate or a mono(2-propanol) solvate.

6. A process of claim 2 wherein the solvent is tetrahydrofuran.

7. A process of claim 6 wherein the solvent is mono(methanol) solvate.

8. A process of claim 6 wherein the solvate is a mono(ethanol) solvate or a mono(2-propanol) solvate.
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