- PHARMACEUTICAL COMPOSITIONS OF (6AS)-6-METHYL-5,6,6A,7-TETRAHYDRO-4H-DIBENZO[DE,G]QUINOLINE-10,11-DIOL
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This invention relates to pharmaceutical compositions for enhancing the solubility of (6aS)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol and salt forms thereof.
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Paragraph 0094-0097
(2021/02/12)
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- PHARMACEUTICAL COMPOSITION FOR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES
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The present invention relates to pharmaceutical compositions for administration to mammals that include (6aS)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient that provides pharmacokinetic profiles useful for the treatment of neurodegenerative diseases.
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Paragraph 0078; 0079; 0080
(2021/02/12)
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- FACILE 'ONE POT' PROCESS FOR APOMORPHINE FROM CODEINE
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An improved method for producing apomorphine and derivatives thereof is provided. The method is a convenient 'one-pot' process, comprising the conversion of codeine into apomorphine without isolating the apocodeine intermediate. Use of water reactive scavengers, reagents that will react irreversibly with water, decreases side product formation and allows the use of milder reaction conditions. This one-pot synthesis of apomorphine from codeine provides a faster reaction with improved yields at temperatures lower as compared to conventional methods. The lower operating temperatures and less volatile reactants make the method particularly useful for large-scale manufacturing.
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Page/Page column 5-6
(2009/04/25)
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- Microwave-promoted acid-catalyzed rearrangement of morphinans - A high-yield synthesis of R(-)-apomorphine
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The microwave-promoted acid-catalyzed rearrangement of morphine (1), codeine (2), and thebaine (3) was investigated. In all cases, a significant improvement in the yields were achieved compared to the traditional techniques. R(-)-Apomorphine (4), which is a clinically important dopamine agonist, was synthesized from morphine (1) in 75% yield. Copyright Taylor & Francis Group, LLC.
- Csutoras,Berenyi,Neumeyer
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p. 866 - 872
(2008/09/17)
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- PROCESS FOR MAKING APOMORPHINE AND APOCODEINE
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There is provided an improved and convenient process for the synthesis of aporphines, such as apomorphine and apocodeine, by the rearrangement of the corresponding morphine or codeine derivatives. The use of a suitable water scavenger in an acid catalyzed rearrangement of the morphine derivatives unexpectedly results in a reaction temperature convenient for plant operation without sacrificing product. The method of the present invention also alleviates the cumbersome operations that were employed in the prior art to eliminate water from the reaction mixture at the elevated temperatures. This process is adaptable for the general preparation of other aporphines from the corresponding morphine congeners.
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Page/Page column 5
(2008/06/13)
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- Aporphines. 27. Mechanistic Aspects of the Rearrangement of Thebaine and Codeine Analogues in Methanesulfonic Acid. Improved Method for Synthesis of N-Alkylated Aporphines
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The rearrangement of thebaine (1a), northebaine (1b), and N-(2-hydroxyethyl)northebaine (1c) in methanesulfonic acid leading to the formation of novel N-alkylated-2-O-methylated normorphothebaine derivatives 4a-c was investigated.We have observed that a s
- Granchelli, Felix E.,Filer, Crist N.,Soloway, Albert H.,Neumeyer, John L.
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p. 2275 - 2278
(2007/10/02)
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