Claims for Patent: 6,020,487

Summary 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.