Amorphous form of apremilast
US-2015283249-A1 · Oct 8, 2015 · US
Forms of apremilast and the process of making the same
US9765026B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9765026-B2 |
| Application number | US-201615246392-A |
| Country | US |
| Kind code | B2 |
| Filing date | Aug 24, 2016 |
| Priority date | Aug 28, 2015 |
| Publication date | Sep 19, 2017 |
| Grant date | Sep 19, 2017 |
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Abstract
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The present invention provides novel crystalline forms of apremilast hemitoluene solvate, apremilast hydrate, and apremilast anhydrate and an amorphous form of apremilast, and processes for the preparation of these forms.
First claim
Opening claim text (preview).
What is claimed is: 1. A process for preparing apremilast, said process comprising: a) contacting (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine and 3-acetamidophthalic anhydride in toluene and acetic acid at elevated temperature to form a mixture; and b) isolating apremilast from the mixture of step a). 2. The process of claim 1 , wherein said elevated temperature is from 80-100° C. 3. The process of claim 1 , wherein said elevated temperature is about 90° C. 4. The process of claim 1 , wherein said apremilast is isolated as apremilast hemitoluene solvate. 5. The process of claim 1 , wherein said isolating comprises filtering the mixture of step a). 6. The process of claim 1 , wherein said toluene and acetic acid are in a ratio of 15/1 to 5/1 (v/v). 7. The process of claim 1 , wherein said toluene and acetic acid are in a ratio of about 7.5/1 (v/v). 8. The process of claim 1 , wherein said apremilast is isolated in >90% yield with >99.5% purity and >99.5% ee.
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Classifications
- C07D209/50Primary
with oxygen and nitrogen atoms in positions 1 and 3 · CPC title
Crystalline forms, e.g. polymorphs · CPC title
Optical isomers · CPC title
- C07D209/48Primary
with oxygen atoms in positions 1 and 3, e.g. phthalimide · CPC title
Isoindoles, e.g. phthalimide · CPC title
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- What does patent US9765026B2 cover?
- The present invention provides novel crystalline forms of apremilast hemitoluene solvate, apremilast hydrate, and apremilast anhydrate and an amorphous form of apremilast, and processes for the preparation of these forms.
- Who is the assignee on this patent?
- Scinopharm Taiwan Ltd
- What technology area does this patent fall under?
- Primary CPC classification C07D209/50. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 19 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).