CAS: 75887-54-6; Arteether

该化合物是来自青蒿素的抗疟化合物,产自青蒿素,摘自白虫木植物Artemisia annua,被归类为一种醚衍生物,主要用于治疗严重疟疾,特别是在观察到抗抗抗疟药物抗药性的情况下;青蒿素表现出迅速的行动,并有效防治最致命的疟疾寄生虫--恶性疟原虫.该化合物通常通过肌肉内注射进行,从而能够快速吸收和在体内传播.青蒿素通过生成反应性氧素物种,损害寄生虫细胞成分,导致其死亡.其致癌性植物基因学涉及较短的半衰期,需要仔细使用和监测.青蒿素一般都受到很好的调适量,但与所有药物一样,它也可能产生副作用,包括潜在的...

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CAS号108739-44-2 3-oxo-8α-hydrox... | CAS号122-51-0 原甲酸三乙酯 | CAS号81496-81-3 α-双氢青蒿素 | CAS号481-05-0 (3S,3aR,4S,5aS,... | CAS号64-17-5 乙醇 | CAS号71939-50-9 双氢青蒿素 | CAS号63968-64-9 青蒿素 | CAS号82596-30-3 脱水二氢青蒿素

合成工艺路线路线简述

  • 合成目标产物 Arteether 主要起始原料 Triethyl Orthoformate And Alpha-Dihydroartemisinin
  • (文献来源)合成步骤主要原料 Triethyl Orthoformate 和 Alpha-Dihydroartemisinin
📜Dihydroartemisinin置于三苯基膦氢溴酸盐,Phosphorus Pentoxide体系中,用 二氯甲烷 作为反应溶剂,化学反应 8.5H,反应生成 蒿乙醚
参考文献:Pu,Yu Ming; Ziffer,Herman,Heterocycles,1994,Vol. 39,# 2,P. 649-656
标题:Pu,Yu Ming; Ziffer,Herman,Heterocycles,1994,Vol. 39,# 2,P. 649-656

海关参考信息

专利信息


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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主要参考文献


1: Looareesuwan S, Oosterhuis B, Schilizzi BM, Sollie FA, Wilairatana P, Krudsood S, Lugt ChB, Peeters PA, Peggins JO. Dose-finding and efficacy study for i.m. artemotil (beta-arteether) and comparison with i.m. artemether in acute uncomplicated P. falciparum malaria. Br J Clin Pharmacol. 2002 May;53(5):492-500.
2: Thuma PE, Bhat GJ, Mabeza GF, Osborne C, Biemba G, Shakankale GM, Peeters PA, Oosterhuis B, Lugt CB, Gordeuk VR. A randomized controlled trial of artemotil (beta-arteether) in Zambian children with cerebral malaria. Am J Trop Med Hyg. 2000 Apr;62(4):524-9. Review. Review. Dutch. doi: 10.1016/j.phymed.2015.08.002. Epub 2015 Aug 18. doi: 10.1007/s00436-015-4321-6. Epub 2015 Jan 25. doi: 10.1038/srep12671.
9: Dhawan S, Gunjan S, Pal A, Tripathi R. Potentiation of antimalarial activity of arteether in combination with Vetiver root extract. Indian J Exp Biol. 2016 May;54(5):315-21. doi: 10.3109/21691401.2014.968821. Epub 2014 Oct 23. doi: 10.4314/ahs.v15i3.19.

合成参考文献


参考文献:10.3109/10408441003610571
摘要:Efferth T, Kaina B. Toxicity of the antimalarial artemisinin and its dervatives. Critical Reviews in Toxicology. 2010 Feb 16;40(5):405–21. doi: 10.3109/10408441003610571.
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