# US 5,703,232 A · Process and solvate of 2-methyl-thieno-benzodiazepine

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- Number: US 5,703,232 A
- Document ID: US5703232A
- Status: Granted
- Kind: A
- Application number: 08/586,431
- Filed: 1996-01-16
- Granted: 1997-12-30
- Earliest claimed: 1995-03-24
- Assignees: Eli Lilly and Company
- Inventors: Charles A. Bunnell; Terrence Michael Hotten; Samuel D. Larsen; David Edward Tupper
- Web page: https://patentgrep.com/patent/US5703232A

## CPC

- C07D 495/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## 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.

## Claims

### Claim 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.

### Claim 2 (depends on 1)

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.

### Claim 3 (depends on 2)

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

### Claim 4 (depends on 3)

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

### Claim 5 (depends on 3)

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

### Claim 6 (depends on 2)

A process of claim 2 wherein the solvent is tetrahydrofuran.

### Claim 7 (depends on 6)

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

### Claim 8 (depends on 6)

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