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ChemicalBook CAS DataBase List Artemether
71963-77-4

Artemether synthesis

13synthesis methods
Artemether is a natural product which effectively kills both malarial parasites P. falciparum and P. vivax. Artemether is usually used in combination with Lumefantrine for the treatment of malaria. Arthemether also kills trematodes of the species Schistosoma, providing protection against schistosomiasis. Sesquiterpene lactones like artemether, artesunate, and artemisinin have potential applications in certain types of cancer and inflammatory conditions.
Synthetic Routes
  • ROUTE 1

    • 202112079961152892.jpg

    Continuous synthesis of artemisinin-derived medicines; Gilmore, Kerry; Kopetzki, Daniel; Lee, Ju Weon; Horvath, Zoltan; McQuade, D. Tyler; Seidel-Morgenstern, Andreas; Seeberger, Peter H. Chemical Communications (Cambridge, United Kingdom); Volume 50; Issue 84; Pages 12652-12655; Journal; 2014

  • ROUTE 2

    • 202112072637181997.jpg

    An Improved Manufacturing Process for the Antimalaria Drug Coartem. Part I; Boehm, Matthias; Fuenfschilling, Peter C.; Krieger, Matthias; Kuesters, Ernst; Struber, Fritz; Organic Process Research & Development; Volume 11; Issue 3; Pages 336-340; Journal; 2007

  • ROUTE 3

    • 202112073810321476.jpg

    Some transition metal complexes bearing artemisinin derivatives and (N-N-O) tridentate chromium (III) complexes ligated by 2-benzolmidazo-yl-6-acetyl-pyridines for catalytic behaviour towards ethylene; Obaleye, Joshua Ayoola; Amolegbe, Saliu Alao; Adewuyi, Sheriff; Sun, Wenhua; Oshodi, Margaret Damilola; Journal of Chemistry and Chemical Engineering; Volume 4; Issue 12; Pages 23-32; Journal; 2010

  • ROUTE 4

    • 202112075333066261.jpg

    Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives; Kopetzki, Daniel; McQuade, David Tyler; Seeberger, Peter H.; Gilmore, Kerry; Assignee Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V., Germany; 2015; Patent Information; Jan 21, 2015; EP 2826779 A1

202112079961152892.jpg

Continuous synthesis of artemisinin-derived medicines; Gilmore, Kerry; Kopetzki, Daniel; Lee, Ju Weon; Horvath, Zoltan; McQuade, D. Tyler; Seidel-Morgenstern, Andreas; Seeberger, Peter H. Chemical Communications (Cambridge, United Kingdom); Volume 50; Issue 84; Pages 12652-12655; Journal; 2014

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Yield:71963-77-4 756 g

Reaction Conditions:

with perchloric acid in dichloromethane at 30 - 38; for 0.166667 h;Large scale;Temperature;

Steps:

1 Example 1

1. examines lost to view complete preparation equipment, equipment clean, ready to complete the original accessories, including the original supplementary product quality detection qualified, filtering, such as the confirmation number.
2. In the reaction, first add dichloromethane 12.8L. Heat to 30 degrees. Afterwards, add dihydroartemisinin 1 kg. After heating under stirring to 38 degrees. Add methanol 4.2L. At the same time, add perchloric acid 200 ml,. At 38 °C, react for 10 minutes; for when the thin chromatographic analysis detection reaction to the end of the, adding anhydrous carbonate sodium accent 0.35K, adjusting PH=7, the termination of the reaction, the reaction liquid filter, to be concentrated.
3. concentrated by filtration of the reaction solution in the 55 °C the left and right water bath concentration to see white the crystal rests stop after precipitation concentrated.
4. crystallization by concentration of the mother liquor after freezing crystallization, centrifugal filtration, add 2L deionized water filtering, to obtain the coarse grain.
5. the refined crystal is added in the 2L of 0.09, stirring 5 minutes, adding 10L60 - 90-range petroleum ether extraction, 60 degrees concentrated to white crystals, tube to saturated solution cooling crystallization, centrifugal filtration, then adding 2L deionized water filtering, high-performance liquid detecting purity of 99.1%.
6. drying and vacuum pressure reducing water bath drying, temperature 50 °C, 120 minutes, high efficiency liquid phase sample detection, the purity is 98.9%, weighing 756g.
7. packaging adopts a double-layer aluminum foil material packing, sealing, completing the label (name, production lot number, date of production and the like), the low-temperature storage.

References:

CN106565738,2017,A Location in patent:Paragraph 0012-0036

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