CAS: 345-78-8; Novafed

该化合物是一种常见的代谢药物,用作场外药物的脱钩剂,其特点是能够通过将血管压缩在鼻腔通道内来缓解鼻塞,从而减少肿胀和堵塞;该化合物一般被发现为白色的,白白的,可溶于水中的晶状粉,并具有一种可方便配制各种药剂的熔点;氢氯甲麻黄碱的分子配方为C10H15NO,分子重量约为185.24克/摩尔;主要对肾上腺受体起作用,导致血管收缩和减少肌肉生产;在有效治疗冷感和过敏症状的同时,该化合物还会产生副作用,如心率上升,在索姆尼亚和...

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上下游产品

((1S,2S)-2-Hydroxy-1-methyl-2-phenyl-ethyl)-methyl-carbamic acid benzyl ester (4S,5S)-4-Methyl-5-phenyl-oxazolidine-3-carboxylic acid benzyl ester (+)-Chloroephedine hydr°Chloride (+)-Chloroephedrine (-)-Chloroephedrine S,2S)-2-methylamino-1-phenyl-propyl ester); hydr°Chlorideacetic acid-((1S,2S)-2-methylamino-1-phenyl-propyl ester); hydr°Chloride Methamphetamin

合成工艺路线路线简述

  • 合成目标产物 (1S,2S)-(+)-Pseudoephedrine Hydrochloride 主要起始原料 3-Oxazolidinecarboxylic Acid, 4-Methyl-5-Phenyl-, Phenylmethyl Ester, (4S,5S)-
  • (文献来源)合成步骤主要原料 3-Oxazolidinecarboxylic Acid, 4-Methyl-5-Phenyl-, Phenylmethyl Ester, (4S,5S)-
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

海关参考信息

专利信息


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.
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主要参考文献


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


摘要:Journal of Pharmacology and Experimental Therapeutics., 71(62), 1941
摘要:Journal of Pharmacology and Experimental Therapeutics., 36(363), 1929
参考文献:10.1007/s00216-012-6600-8
摘要:NicDaéid N, Jayamana S, Kerr WJ, Meier-Augenstein W, Kemp HF. Influence of precursor solvent extraction on stable isotope signatures of methylamphetamine prepared from over-the-counter medicines using the Moscow and Hypophosphorous routes. Analytical and Bioanalytical Chemistry. 2012 Dec 15;405(9):2931–41. doi: 10.1007/s00216-012-6600-8.
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