坦索洛新置于盐酸体系中,用 乙醇 用作溶剂,化学反应 4.0H,反应生成盐酸坦索罗辛 参考文献: Synthesis Of Optically Pure (R)-5-(2-Aminopropyl)-2-Methoxybenzenesulphonamide[fr] Synthese De (R)-5-(2-Aminopropyl)-2-Methoxybenzenosulfonamide Optiquement Pur 标题: Synthesis Of Optically Pure (R)-5-(2-Aminopropyl)-2-Methoxybenzenesulphonamide[fr] Synthese De (R)-5-(2-Aminopropyl)-2-Methoxybenzenosulfonamide Optiquement Pur 摘要:本发明涉及一种制备光学纯(R)-5-(2-氨丙基)-2-甲氧基苯磺胺的新工艺,该化合物是特拉唑嗪合成中的中间体.
专利信息
专利号:US-8193384-B2 优先权日:2005-07-29 标 题 :Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds 发明人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF 权利人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF; RHODE ISLAND EDUCATION 摘要:The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.
专利号:US-2024158926-A1 优先权日:2022-11-03 标 题 :Electrochemical synthesis of hydroxyvaleric acid from levulinic acid 发明人:HOLEWINSKI ADAM; DE SOUZA LUCAS FRANCISCO WILLIAN 权利人:UNIV COLORADO REGENTS 摘要:Disclosed herein are methods of electrochemical synthesis of hydroxyvaleric acid from levulinic acid. For example, disclosed herein are methods comprising electrochemical synthesis of hydroxyvaleric acid from levulinic acid, wherein the method is conducted in an electrochemical cell wherein a working electrode is in electrochemical contact with an aqueous electrolyte and levulinic acid, wherein the method comprises applying a potential to electrochemically reduce the levulinic acid to form hydroxyvaleric acid. Also disclosed herein are methods of synthesizing gamma-valerolactone from hydroxyvaleric acid, the method comprising acid-catalyzed esterification. Also disclosed herein are methods of use of the products produced by any of the methods herein.
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-7619116-B2 优先权日:2003-12-17 标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation 发明人:DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM 权利人:PRODUCTS CHIMIQUES AUXILIAIRES 摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.
专利号:US-7538246-B2 优先权日:2003-12-29 标 题:Synthesis of optically pure(r)-5-(2-amynopropyl)-2-methoxybenzenesulphonamide 发明人:MOHAR BARBARA 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to a new process for the preparation of optically pure(R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide, which is an intermediate in the synthesis of tamsulosin.
专利号:US-11713331-B2 优先权日:2020-04-12 标 题 :Benzene 1,4-bis(bisphosphonic acid)-based metal complexes, method of synthesis and applications thereof 发明人:LOPEZ-MEJIAS VILMALI; CARMONA-SARABIA LESLY Y; ESCALERA JOY ANDREA M; MOJICA VAZQUEZ DARILYS 权利人:LOPEZ MEJIAS VILMALI; CARMONA SARABIA LESLY Y; ESCALERA JOY ANDREA M; MOJICA VAZQUEZ DARILYS; UNIV PUERTO RICO 摘要:The invention provides extended bisphosphonate-based metal complexes using benzene1,4-bis(bisphosphonic acid) (BBPA), an analog of benzene 1,4-dicarboxylic acid (BDC). Hydrothermal synthesis of BBPA with the bioactive metals Ca 2+ , Zn 2+ , and Mg 2+ leads to four crystals phases, namely, BBPA-Ca forms I and II, BBPA-Zn form I, and BBPA-Mg form I. Out of the three structures, BBPA-Ca form II presents large channels (8 Å×12 â„«), potentiating the use of this framework to load drugs. Cytotoxicity effects of BBPA was elucidated in a human breast cancer MDA-MB-231 and a normal osteoblast hFOB 1.19 cell lines. The half-maximal inhibitory concentration (IC 50 ) for BBPA used to treat both cell lines were >200 μM at 24, 48, and 72 h of treatment. The BBPA in the range of concentration employed (0-200 μM) was not cytotoxic against these cell lines.
1: Fossler MJ, Collins DA, Thompson MM, Nino A, Bianco JJ, Chetty D. Pharmacokinetic bioequivalence studies of a fixed-dose combination of tamsulosin and dutasteride in healthy volunteers. Clin Drug Investig. 2014 May;34(5):335-49. doi: 10.1007/s40261-014-0179-0. doi: 10.1016/j.ijpharm.2013.06.065. Epub 2013 Jul 5. doi: 10.1016/j.urology.2013.03.026. Epub 2013 May 25. Epub 2012 May 15. 5: Kumari R, Dash PP, Lal VK, Mishra A, Murthy PN. RP - HPLC method for the estimation of Tamsulosin Hydrochloride in Tablet Dosage Form. Indian J Pharm Sci. 2010 Nov;72(6):785-7. doi: 10.4103/0250-474X.84596. 6: Korstanje C, Krauwinkel W, van Doesum-Wolters FL. Tamsulosin shows a higher unbound drug fraction in human prostate than in plasma: a basis for uroselectivity? Br J Clin Pharmacol. 2011 Aug;72(2):218-25. doi: 10.1111/j.1365-2125.2010.03870.x.
合成参考文献
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