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US 9,428,444 B2Granted
Process for the preparation of levothyroxine sodium
AssigneeAzico Biophore India Private Limited
InventorsCh. A. P. Rameswara Rao, Sreenath Dasari
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Abstract
The present invention provides a novel process for the preparation of highly pure Levothyroxine Sodium, i.e., (S)-2-amino-3-[4-(4-hydroxy-3, 5-diiodophenoxy)-3,5-diiodophenyl] propanoic acid sodium salt via two process intermediates viz 3,5-Diiodo L-Tyrosine copper complex and novel Bis (p-anisyl) iodonium Iodide. The invention also provides levothyroxine pentahydrate free from genotoxic impurities and liothyronine levels below 0.04% wt/wt.
Claims2
A process for the preparation of Levothyroxine Sodium comprising the steps of:
- a. Coupling reaction between 3, 5-diiodo L-Tyrosine copper complex and novel Bis (p-anisyl) iodonium iodide in the presence of Diisopropylamine or other organic bases in n-Butanol or other alcoholic solvents to obtain 2-Amino-3-(3,5-diiodo-4-(4-methoxy phenoxy)phenyl)propanoic acid;
- b. Demethylation of 2-Amino-3-(3,5-diiodo-4-(4-methoxyphenoxy)phenyl)propanoic acid using a mixture of Acetic acid and Hydroiodic acid to obtain 3,5-diiodothyronine;
- c. Iodinizing 3,5-diiodothyronine with methanolic or alcoholic monomethylamine and Iodine to obtain Levothyroxine;
- d. Converting Levothyroxine to Levothyroxine Sodium in the presence of sodium hydroxide and n-butanol or other alcoholic solvents.
1 more element
Dependencies are inferred from the claim text.