蒿甲醚相关物质b置于三甲基氯硅烷体系中,用 甲苯 作为反应溶剂,化学反应 12.0H,反应生成 蒿甲醚 参考文献: A Process For Preparation Of Ether Derivatives Of Dihdroartemisinin[fr] Procédé De Préparation De Dérivés éther De La Dihydroartémisinine 标题: A Process For Preparation Of Ether Derivatives Of Dihdroartemisinin[fr] Procédé De Préparation De Dérivés éther De La Dihydroartémisinine
专利号:US-7947701-B2 优先权日:2003-11-14 标题:Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof 发明人:CAZELLES JEROME; COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN 权利人:SANOFI AVENTIS 摘要:The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.
专利号:US-9802952-B2 优先权日:2013-07-15 标 题:Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives 发明人:KOPETZKI DANIEL; MCQUADE DAVID TYLER; SEEBERGER PETER H; GILMORE KERRY 权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V; MAX-PLANK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V 摘要:The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C 1 -C 5 alcohol.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-9382288-B2 优先权日:2010-10-06 标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action 发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO 权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG 摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
专利号:WO-2008087666-A1 优先权日:2007-01-19 标 题:Preparative process for ether derivative of artemisinin 发明人:DEGANI MARIAM S; NARKHEDE SACHIN S; PEDGAONKAR YOGESH Y; CHAVAN SUNIL S 权利人:ALMET CORP; DEGANI MARIAM S; NARKHEDE SACHIN S; PEDGAONKAR YOGESH Y; CHAVAN SUNIL S 摘要:The present invention relates to a process for synthesis of ether derivative of artemisinin by reducing artemisinin to dihydroartemisinin using a mixture of sodium borohydride and a dihydroxy compound, followed by etherification in presence of an acid catalyst and an alcohol.
专利号:US-2006287257-A1 优先权日:2005-06-20 标 题 :Pharmaceutical compositions to treat diseases caused by mycobacterium 发明人:STOCKEL RICHARD F 权利人:STOCKEL RICHARD F 摘要:The invention teaches the synthesis of pharmaceutical composition and methods of synthesis to treat people and animals infected with a pathogenic mycobacterium. In particular the compositions of this invention are suitable for the treatment of tuberculosis, malaria, and other infections diseases caused by mycobacterium.
1: Swain TR, Raulo A, Mohapatra N, Singha MR. Information Education and Communication can Improve Adherence to Artemether-Lumefantrine Combination in Patients of Uncomplicated Falciparum Malaria. J Clin Diagn Res. 2015 Sep;9(9):FC01-3. doi: 10.7860/JCDR/2015/13196.6544. Epub 2015 Sep 1. doi: 10.1186/s12916-015-0456-7. 4: Gray AM, Arguin PM, Hamed K. Surveillance for the safety and effectiveness of artemether-lumefantrine in patients with uncomplicated Plasmodium falciparum malaria in the USA: a descriptive analysis. Malar J. 2015 Sep 17;14:349. doi: 10.1186/s12936-015-0881-2. 5: Yavo W, Konaté A, Kassi FK, Djohan V, Angora EK, Kiki-Barro PC, Vanga-Bosson H, Menan EI. Efficacy and Safety of Artesunate-Amodiaquine versus Artemether-Lumefantrine in the Treatment of Uncomplicated Plasmodium falciparum Malaria in Sentinel Sites across Côte d'Ivoire. Malar Res Treat. 2015;2015:878132. doi: 10.1155/2015/878132. Epub 2015 Aug 12.
合成参考文献
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