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-5171676-A 优先权日:1991-10-31 标 题 :Method of introducing hydroxyl groups into artemisinin and its derivatives 发明人:ZIFFER HERMAN; HU YULIN 权利人:US HEALTH 摘要:The fungus Beauveria sulfurescens has been employed to introduce hydroxyl groups into artemisinin and derivatives of artemisinin, an antimalarial. Hydroxylated derivatives of artemisinin and derivatives of artemisinin produced thereby possess antimalarial activity, and can serve as intermediates in the synthesis of further derivatives useful in treating malaria.
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-5011951-A 优先权日:1988-02-25 标题:Synthesis of artemisininelactol derivatives 发明人:BUCHS PETER; BROSSI ARNOLD 权利人:WORLD HEALTH ORG 摘要:A process for the epimerization of α- to β-ethyletherartemisininelactol (arteether) or preparation of arteether, useful in the treatment of malaria, from artemisininelactol, comprises reacting starting material in a solvent including an acid catalyst, the reaction of artemisininelactol also including an etherifying ethyl moiety, and isolating the product.
专利号:US-9006467-B2 优先权日:2011-02-14 标题:1,2,3-triazole containing artemisinin compounds and process for preparation thereof 发明人:SAIKIA BISHWAJIT; BARUA NABIN C; SAIKIA PARTHA P; GOSWAMI ABHISHEK; RAO PARUCHURI G; SAXENA AJIT K; SURI NITASHA 权利人:SAIKIA BISHWAJIT; BARUA NABIN C; SAIKIA PARTHA P; GOSWAMI ABHISHEK; RAO PARUCHURI G; SAXENA AJIT K; SURI NITASHA; COUNCEL OF SCIENT & IND RES 摘要:The present invention relates to 1,2,3-triazole containing artemisinin compounds and process for preparation thereof. Described herein is the synthesis, bioassay results and usefulness of the artemisinin derived compounds resulting from 1,3-dipolar cycloaddition reaction of artemisinin derived azide or alkyne with aliphatic or aromatic diazides. These 1,2,3-triazole containing artemisinin derived compounds embodied in this document are found to be active against various cancer cell-lines.
专利号:CN-1028294-C 优先权日:1989-12-21 标题:Synthesis of a Class of Nitrogen-Containing Artemisinin Derivatives
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合成参考文献
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