- Improved method for synthesizing L-thyroxine sodium
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The invention relates to an improved method for synthesizing L-thyroxine sodium. The improved method includes the steps that 3,5-diiodomethane-L-tyrosine is used as a raw material, and then subjectedto a copper complex reaction, a coupling reaction, an acid hydrolysis reaction, an iodine generation reaction and a salt forming reaction to obtained the L-thyroxine sodium. According to the improvedmethod for synthesizing the L-thyroxine sodium, the yield of the L-thyroxine sodium can be improved, the product cost is lowered, and industrialization is convenient.
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- Liquid levothyroxine formulations
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Embodiments of the present invention provide levothyroxine solutions that consist of from about 0.001% w/v to about 0.01% w/v of a levothyroxine; at least 70% w/w of a glycerol; less than 30% w/w of a water; and from about 0.01% w/w to about 1.5% w/w of an ethylenediaminetetraacetic acid (EDTA). Such levothyroxine solutions are characterized by exhibiting levothyroxine storage stability.
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- NOVEL PROCESS FOR THE PREPARATION OF LEVOTHYROXINE SODIUM
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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 lodide.The invention also provides levothyroxine pentahydrate free from genotoxic impurities and liothyronine levels below 0.04% wt/wt.
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- A PROCESS FOR PREPARATION OF LEVOTHYROXINE AND SALTS THEREOF
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The present invention relates to a process for the preparation of Levothyroxine and salts thereof. The process described in the present invention provides increase in the yields and purity comprising the use of sodium iodide and sodium hypochlorite as iodinating agent.
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Page/Page column 14
(2015/11/30)
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- The synthesis of 13C9-15N-labeled 3,5-diiodothyronine and thyroxine
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Thyroid hormones undergo extensive metabolism to regulate hormone activity. A labeled thyroid hormone would be useful to track hormone metabolism through various pathways. While radiolabeled thyroid hormones have been synthesized and used for in vivo studies, a stable isotope labeled form of thyroid hormone is required for studying thyroid hormone metabolism by LC-MS/MS, an analytical technique that has certain advantages without the complications of radioactivity. Here we report the synthesis of 13C9- 15N-T2 and 13C9-15N- T4, two labeled thyroid hormone derivatives suitable for in vivo LC-MS/MS studies. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file.
- Hackenmueller, Sarah A.,Scanlan, Thomas S.
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p. 1439 - 1446
(2013/05/22)
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- COMPOSITIONS AND METHODS FOR CYCLOFRUCTANS AS SEPARATION AGENTS
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The present invention relates to derivatized cyclofructan compounds, compositions comprising derivatized cyclofructan compounds, and methods of using compositions comprising derivatized cyclofructan compounds for chromatographic separations of chemical species, including enantiomers. Said compositions may comprise a solid support and/or polymers comprising derivatized cyclofructan compounds.
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Page/Page column 45-49; 61
(2010/12/31)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF LEVOTHYROXINE SODIUM WITH REDUCED LEVELS OF IMPURITIES
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The invention relates to an improved process for the preparation of Levothyroxine sodium with reduced levels of impurities. The invention also provides Levothyroxine sodium pentahydrate free from 3,5-Diiodothyronine or d-enantiomer of thyroxine. The invention also provides Levothyroxine sodium pentahydrate having liothyronine below 0.5% wt / wt.
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Page/Page column 5
(2010/01/29)
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- Thyroxine/cyclodextrin complexes and pharmaceutical compositions containing the same
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Thyroxine containing pharmaceutical compositions with improved aqueous solubility, stability and enhanced membrane permeation have been prepared by formulating thyroxine with cyclodextrins. These thyroxine/cyclodextrin complexes can further be transformed into different dosage forms (oral tablets, injectables, transdermal patches, hydrogels, ointments, suppositories etc.) by employing known, common pharmaceutical additives.
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- Iodothyronine polymers
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Iodothyronine polymers having a plurality of recurring units of formula I STR1 in which A is iodo and B, C and D are independently H or iodo are described. Polymers in which A and C are iodo and B and D are independently H or iodo and in which substantially all of the recurring units are L-stereoisomers, have utility in treating thyroid hormone deficiencies.
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- A concise synthesis of thyroxine (T4) and 3,5,3'-Triiodo-L-thyronine (T3)
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The mono- and di-iodo derivatives of 1-oxaspiro[2,5]bicycloocta-4,7-dien-6-one, 8 and 9, reacted readily with 3,5-diiodo-L-tyrosine at pH 8.0 to give 3,5,3'-triiodo-L-thyronine (T3) and thyroxine in 70% and 94% yields respectively. In turn, 8 and 9 were prepared by the sodium bismuthate oxidation of their corresponding iodinated p-hydroxybenzyl alcohol derivatives, 6 and 7 in 32% and 37% yields.
- Salamonczyk, Grzegorz M.,Oza, Vibha B.,Sih, Charles J.
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p. 6965 - 6968
(2007/10/03)
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- Sata and other thiol precursors
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The present invention is directed to methods for using reagents to generate and stabilize thiols derived from thiol precursors in order to permit more effective reactions with thiol-reactive substances such as liposomes, proteins and antibodies. These methods provide greatly improved conjugates for utilization in various in vivo and in vitro applications.
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- Conjugates
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A compound represented by the formula STR1 wherein X is a spacer group. The compound is useful for conjugating a compound having an alcohol group or an amine group to a compound having a thiol group. The compound can be used to conjugate a biologically active group such as an antigen to a protein such as an enzyme to provide an enzyme-labeled antigen for use in enzyme-amplified immunoassay methods for analytes or metabolites in sample fluids. The compound can also be used to immobilize a material such as a protein to a solid support.
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- Reagents and methods for the detection and quantification of thyroxine in fluid samples
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Immunoassay methods and reagents for the specific quantification of thyroxine in a test sample are disclosed employing antibodies prepared with thyroxine derivatives of the formula: STR1 wherein P is an immunogenic carrier material and X is a linking moiety. The present invention also describes the synthesis of unique labelled reagent of the formula: STR2 wherein Q is a detectable moiety and W is a linking moiety, preferably fluorescein or a fluorescein derivative.
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