Benzyl N-[(1S,2S)-1-Hydroxy-1-Phenylpropan-2-Yl]-N-Methylcarbamate置于盐酸体系中,化学反应 2.0H,以92%的收率获得产物盐酸伪麻黄碱 参考文献:An Enantioselective Synthesis Of (1S,2S)-Pseudoephedrine 标题:An Enantioselective Synthesis Of (1S,2S)-Pseudoephedrine 摘要:Synthesis Of (1S,2S)-Pseudoephedrine Is Described Via Reduction Of An Alanine-Derived Oxazolidinone Followed By Treating With Phenyl Magnesium Bromide And Chemoselective N-Methylation In An Efficient And Practical Manner. (C) 2000 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0040-4039(99)02106-1
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:WO-2005105153-A1 优先权日:2004-04-30 标 题 :Hydroxyalkyl derivatives of biologically active compounds 发明人:DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL 权利人:KOPRAN RES LAB LTD; DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL 摘要:Hydroxyalkyl derivatives of biologically active compounds represented by the formula VII wherein R2 = H, CI-12 alkyl, C6-12 aryl, or -OH and D = Biologically active agent having functional groups such as Formula (a) epoxy or aziridine and Z' = Formula (b) L= spacer comprising (un)substituted alkyl, hydroxyalkyl or alkoxy alkyl with the condition that the carbon chain length contains 2 to 6 carbon atoms when Z' = Formula (c) and pharmaceutically acceptable acid addition salts and enantiomers thereof Also process for the synthesis of compounds of the Formula VII and pharmaceutically acceptable acid addition salts and enantiomers thereof comprising condensation of the biologically active agents having functional groups such as Formula (d) epoxy or azifidine with substituted alkyl derivatives under alkaline conditions, at 20 - 80°C, in an organic solvent.
专利号:US-11617758-B2 优先权日:2009-12-31 标 题 :Emulsion formulations 发明人:DHINGRA OM; BERNSTEIN JAMES S 权利人:MARIUS PHARMACEUTICALS LLC 摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-2013303495-A1 优先权日:2009-12-31 标题:Emulsion formulations 发明人:DHINGRA OM; BERNSTEIN JAMES S 权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC 摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-2025002508-A1 优先权日:2020-05-05 标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof 发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS 权利人:QPEX BIOPHARMA INC 摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
专利号:US-2005053642-A1 优先权日:2000-08-23 标题:Biocompatible materials 发明人:ULBRICHT MATHIAS; THOM VOLKMAR; JANKOVA KATJA; ALTANKOV GEORGE; JONSSON GUNNAR 摘要:The present invention teaches a novel approach of creating biocmpatible surfaces, said surfaces being capable of functionally interact with biological material. SAid biocompatible surfaces comrise at least two comonents, such as a hydrophobic substratum and a macromolecule of hydrophilic nature, which, in a cooperativity, form together the novel biocoompatible surfaces. The novel approach is ased on contacting said hydrophobic substratum with a laterally patterned monomolecular layer of said hydrophilic and flexible macromolecules, exhibiting a pronounced excluded volume. The htus formed two component surface is, in respect to polarity and morphology, a molecularly heterogeneous surface. Structural features of said macromolecular monolayer (as e.g. the layer thickness or its lateral density) are determined by: i) the structural features of the layer forming macromolecules (as e.g. their MW or their molecular architecture) and ii) the method of creating said monomolecular layer (as e.g. by physi- or chemisorbing, or by chemically binding said macromolecules). The structural features of the layer forming macromolecules(s) is in turn determined by synthesis. AMount and conformation and thus also biological activity of biological material (as e.g. polypeptides) which contact the novel biocompatible surface, is determined and maintained by the cooperative action of the underlying hydrophobic substratum and the macromolecular layer. In this way it becomes possible to maintain and control biological interactions between said contacted polypeptides and other biological compounds as e.g. cells, antibodies and the like. Consequently, the present invention aims to reduce and/or eliminate the deactivation and/or denaturation associated with the contacting of polypeptides and/or other biological material to a hydrophobic substratum surface.
1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Pseudoephedrine. 2025 Sep 20. 40(12):2125-2137. doi: 10.1080/03007995.2024.2424422. Epub 2024 Nov 12. 1994–. Pseudoephedrine. 2024 Mar. 43(1):325-342. doi: 10.1111/dar.13777. Epub 2023 Nov 14. 22(10):5146. doi: 10.3390/ijms22105146. 6: Munafò A, Frara S, Perico N, Di Mauro R, Cortinovis M, Burgaletto C, Cantarella G, Remuzzi G, Giustina A, Bernardini R. In search of an ideal drug for safer treatment of obesity: The false promise of pseudoephedrine. Rev Endocr Metab Disord. 2021 Dec;22(4):1013-1025. doi: 10.1007/s11154-021-09658-w. Epub 2021 May 4. 7: Chiarugi A, Camaioni A. Update on the pathophysiology and treatment of rhinogenic headache: focus on the ibuprofen/pseudoephedrine combination. Acta Otorhinolaryngol Ital. 2019 Feb;39(1):22-27. doi: 10.14639/0392-100X-1882.
合成参考文献
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