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Claims for Patent: 6,020,487

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Claims for Patent: 6,020,487

Title: Intermediates and process for preparing olanzapine
Abstract:The present invention provides a process for preparing olanzapine and intermediates therefor.
Inventor(s): Bunnell; Charles Arthur (Lafayette, IN), Larsen; Samuel Dean (West Lafayette, IN), Nichols; John Richard (Merseyside, GB), Reutzel; Susan Marie (Indianapolis, IN), Stephenson; Gregory Alan (Fishers, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:08/935,884
Patent Claims: 1. An olanzapine dihydrate selected from Dihydrate B and Dihydrate E.

2. A dihydrate of claim 1 which is crystalline Dihydrate B and which has a typical X-ray powder diffraction pattern with the following interplanar spacings (d) in Angstroms:

3. A Dihydrate B of claim 2 wherein the diffraction pattern has the following typical relative intensity (I/I.sub.1) pattern:

4. A Dihydrate B of claim 3 in substantially pure form.

5. A dihydrate of claim 1 which is crystalline Dihydrate E and which has a typical X-ray powder diffraction pattern with the following interplanar spacings (d) in Angstroms:

6. A Dihydrate E of claim 5 wherein the diffraction pattern has the following typical relative intensity pattern (I/I.sub.1):

7. A Dihydrate E of claim 6 in substantially pure form.

8. A process for preparing substantially pure Form II olanzapine comprising preparing an olanzapine dihydrate selected from Dihydrate B, Dihydrate D and Dihydrate E and drying it until the Form II is prepared.

9. A process of claim 8 wherein the dihydrate is dried in a vacuum oven at about 40.degree. C. to about 70.degree. C.

10. A process of claim 9 wherein the dihydrate is Dihydrate D.

11. A process of claim 9 wherein the dihydrate is Dihydrate B.

12. A process of claim 9 wherein the dihydrate is Dihydrate E.
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