|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|
|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.