Process and solvate of 2-methyl-thieno-benzodiazepine
AssigneesEli Lilly and Company, Lilly Industries Limited
InventorsCharles A. Bunnell, Terrence M. Hotten, Samuel D. Larsen, David E. Tupper
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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 solyates of olanzapine. The invention provides a method for using such solyates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.
Claims10
A crystalline mono methanol solvate form of a compound of the Formula I ##STR3##
A crystalline mono ethanol solvate form of a compound of the Formula I ##STR4##
A crystalline mono 1-propanol solvate form of a compound of the Formula I ##STR5##
A process for preparing a lower alcohol solvate comprising preparing technical olanzapine which comprises contacting intermediate 1 ##STR6## with dimethylsulfoxide and N-methylpiperazine with heating at about 90.degree. C. to about 130.degree. C.;
- and
- crystallizing olanzapine from the reaction mixture with a solvent selected from the group consisting of lower alcohols to provide the corresponding lower alcohol solvate of olanzapine.
Dependencies are inferred from the claim text.