- GEMCITABINE PRODRUGS
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Provided herein are phosphorylated gemcitabine derivative prodrug compounds, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of cancer.
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Paragraph 00170; 00173
(2020/11/12)
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- Proline derivatives incorporating hydrophobic long-chain derived from natural and synthetic fatty acids
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The α-hydrophobic long chain-α-amino esters are prepared by α-hydroxylation of a series of fatty acid esters [derived from oleic acid (OA), linoleic acid (LA), arachidonic acid (ARA) and docosahexaenoic acid (DHA)] followed by Mitsunobu reaction and hydrazinolysis of the phthalimide. These amino esters are mixed with aldehydes and electrophilic alkenes to give very good chemical yields and diastereoselectivities of prolinate derivatives incorporating a hydrophobic long chain at the α-position. This multicomponent 1,3-dipolar cycloaddition (1,3-DC) takes place at room temperature. The synthesis of the homologue hydrophobic chain of OA is performed by its oxidation to aldehyde/racemic N-tert-butylsulfinyl imine/Neff reaction. Final 1,3-DC with benzaldehyde and N-methylmaleimide affords homologue prolinate derivative in good yield.
- Selva, Elisabet,Soto, J. Javier,Nájera, Carmen,Foubelo, Francisco,Sansano, José M.
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p. 1378 - 1386
(2019/02/05)
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- Preparation of n-3 PUFAs ethyl esters by an efficient biocatalyzed solvent-free process
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alpha-Linolenic acid (ALA), eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) have been subjected to esterification with ethanol in presence of lipase B from Candida antarctica (Novozym 435), in solvent free condition. The use of alcohol donors triethyl orthoformate (TEOF) or diethyl carbonate (DEC) instead of free ethanol, allowed working in irreversible esterification conditions and ALA-, EPA- and DHA-ethyl esters were obtained in quantitative yields.
- Morrone,D'Antona,Biondi,Lambusta,Nicolosi
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p. 173 - 176
(2012/11/06)
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- METHODS OF PREPARING FREE POLYUNSATURATED FATTY ACIDS
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Provided herein are methods of making compositions of free fatty acids and alkyl esters of polyunsaturated fatty acids (PUFAs). Also provided are compositions comprising a PUFA selected from a free fatty acid or a ester wherein the PUFA is made according to a method of the invention.
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Page/Page column 29
(2012/09/10)
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- Compositions and methods of omega polyunsaturated fatty acids for the treatment of oral diseases
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The invention discloses a novel discovery of anti-microbial activity against oral bacteria, which can be applied for controlling and preventing oral diseases, of omega-3, omega-6, and omega-9 fatty acids, but not limited to omega-3, omega-6, and omega-9 fatty acids; omega-3, omega-6, and omega-9 fatty acid methyl esters, and omega-3, omega-6, omega-9 fatty acid ethyl esters and their application method. The application of this discovery includes the preparation of drugs, dietary supplements, food and daily necessities with oral health care and therapeutic effects.
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Page/Page column 2-3
(2011/05/05)
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- Process for the preparation of a composition comprising unsaturated compounds
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The present invention relates to a process for the preparation of a composition comprising unsaturated compounds, in particular polyunsaturated compounds, which comprises concentrating and purifying the compounds by contact with silicon and/or aluminium derivatives. The process of the invention represents an advantageous substitute of the usual distillation processes, coupled or not to chromatographic processes, and allows to isolate and remove polar byproducts.
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Page/Page column 5
(2008/06/13)
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- LIPASE-CATALYSED ESTERIFICATION OF MARINE OIL
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Marine oil compositions which contain EPA and DHA as free acids or hexyl esters are esterified with ethanol in the presence of a lipase catalyst under essentially organic solvent-free conditions and separated by distillation.
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- New Synthon for the Convergent Construction of Skipped Conjugation Polyenes: Synthesis of Ethyl Docosa-4,7,10,13,16,19-hexaenoate
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The preparation and subsequent Wittig reaction of the (Z,Z)-phosphonium salt 4, a useful synthon for the preparation of skipped conjugation polyenes, are reported.Salt 4 is a key intermediate for the synthesis of ethyl docosa-4,7,10,13,16,19-hexaenoate (3
- Taber, Douglass F.,You, Kamfia
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p. 139 - 142
(2007/10/02)
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