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ChemicalBook CAS DataBase List Apremilast

Apremilast synthesis

2synthesis methods
1384440-16-7 Synthesis
Apremilast

1384440-16-7
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Apremilast

1384439-80-8
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Yield:-

Reaction Conditions:

with aluminum (III) chloride in dichloromethane at 20; for 1 h;

Steps:

5.9

5.9 (S)-4-Amino-2-[1-(3,4-dihydroxy-phenyl)-2-methanesulfonyl-ethyl]-isoindole-1,3-dione To a stirred solution of (S)-4-amino-2-[1-(3-ethoxy-4-hydroxy-phenyl)-2-methanesulfonyl-ethyl]-isoindole-1,3-dione (0.55 mmol) in anhydrous CH2Cl2 at room temperature, is added AlCl3 (2.2 mmol). After stirring for 1 hour, water is added. The product is extracted into CH2Cl2, and the organic extract is dried over MgSO4. The solvent is removed to afford crude (S)-4-amino-2-[1-(3,4-dihydroxy-phenyl)-2-methanesulfonyl-ethyl]-iso indole-1,3-d lone. The product is purified by column chromatography or recrystallization.

References:

US2012/178708,2012,A1 Location in patent:Page/Page column 21

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