AUTHOR OF THIS BLOG

DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER
Jan 012015
 

IMAGE……….http://www.laboratorytalk.com/life-sciences-and-clinical-laboratory-equipment/synthesis-systems/flow-chemistry-system-aids-synthesis-of-cns-drugs/404882.article

 

 

1…………………

 

Gleevec, developed by Novartis, is a tyrosine kinase inhibitor used for the treatment of chronic myeloid leukaemia and gastrointestinal stromal tumours. The drug molecule represents a particularly challenging target for flow chemistry because of the low solubility of many of the reaction components required for its synthesis. The team devised a new synthesis route that prevents the equipment blockages from product precipitation and avoids many of the labour and time intensive practices of traditional batch-based preparation.

 

flow synthesisThe flow-based route required minimal manual intervention and was achieved despite poor solubility of many reaction componentsLINK………...http://www.rsc.org/chemistryworld/2013/01/flow-synthesis-anticancer-drug

2…………………..

Malaria is a serious global health issue. Artemisinin combination treatments are the first-line drugs, but supplies are limited because artemisinin is obtained solely by extraction from Artemisia annua. A continuous-flow process that converts dihydroartemisinic acid into artemisinin (see scheme) was shown to be an inexpensive and scalable process that can ensure a steady, affordable supply of artemisinin.

Continuous-Flow Synthesis of the Anti-Malaria Drug Artemisinin

  1. Dr. François Lévesque1 and
  2. Prof. Dr. Peter H. Seeberger1,2,*

Article first published online: 16 JAN 2012

DOI: 10.1002/anie.201107446………….http://onlinelibrary.wiley.com/doi/10.1002/anie.201107446/abstract

 

 

IMAGE………..http://phys.org/news/2013-08-chemists-fresh-approach-alloy-nanomaterials.html

 

 

 

3……………….

 

http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-9-265

 

 

IMAGE……..http://www.chemistryviews.org/details/ezine/1058453/Women_in_ChemistryA_European_Journal.html

 

 

4…………………….

 

http://www.rsc.org/chemistryworld/2014/09/antimalarial-flow-synthesis-commercialisation-artemisinin

 

 

 

 

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http://pipeline.corante.com/archives/2014/04/

 

http://www.chemistryviews.org/details/ezine/5753931/Liliana_Mammino_Research_and_Education_in_Sub-Saharan_Africa.html

 

 

 

6…………………………

http://pubs.rsc.org/en/content/articlelanding/2013/ob/c2ob27003j#!divAbstract

 http://www.amnh.org/learn-teach/young-naturalist-awards/winning-essays2/2013-winning-essays/optimizing-algae-biofuels-applied-natural-selection-to-improve-lipid-synthesis

 

 

 

7…………………..

 

http://onlinelibrary.wiley.com/doi/10.1002/anie.201305429/abstract

http://www.rsc.org/chemistryworld/2012/04/iron-lady

 

 

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http://www-medchem.ch.cam.ac.uk/hot_topics.php

http://www.ollusa.edu/s/1190/ollu.aspx?pgid=2674

 

 

 

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http://www.mdpi.com/1420-3049/19/7/9736

http://www.ed.ac.uk/alumni/services/news/news/femalechemists

 

 

 

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http://newdrugapprovals.org/2014/12/31/continuous-flow-synthesis-of-alpha-halo-ketones-building-blocks-for-anti-retroviral-agents/

main image

 

http://www3.imperial.ac.uk/newsandeventspggrp/imperialcollege/newssummary/news_26-9-2013-11-6-53

 

 

 

 

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http://pubs.rsc.org/en/content/articlehtml/2013/ob/c3ob41464g

 

http://emmittnlxe.soup.io/

 

 

 

 

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http://pubs.rsc.org/en/content/articlelanding/2012/sc/c2sc21850j#!divAbstract

 

IMAGE……..http://evnewsreport.com/tag/battery/

 

 

 

 

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http://www.leygroup.ch.cam.ac.uk/research/continuous-flow-methodology/heterocycles-flow

IMAGE……….http://www.chemistryviews.org/details/ezine/1059875/Women_in_Chemistry__Interview_with_Zeinab_Shaaban_Abd_El-Ati_Abou_El-Naga.html

 

 

 

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http://www.sfu.ca/chemistry/groups/britton/publications.html

 

 

 

IMAGE……….http://www.greentechnolog.com/green_chemistry/

 

 

 

 

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RUFINAMIDE….FLOW SYNTHESIS

 SYNTHESIS  Comments Off on RUFINAMIDE….FLOW SYNTHESIS
Jan 012015
 

A report (Org Process Res Dev 2014, ASAP article) out of Jamison’s group at MIT, provides a 3-step synthesis of Rufinamide in 92% overall yield. The process illustrates a continuous and convergent method, moving away from the isolation of a key organic azide intermediates and a Cu coiled-tube reactor for the cycloaddition reaction to the corresponding desired triazole.

http://pubs.acs.org/doi/abs/10.1021/op500166n

Small molecules bearing 1,2,3-triazole functionalities are important intermediates and pharmaceuticals. Common methods to access the triazole moiety generally require the generation and isolation of organic azide intermediates. Continuous flow synthesis provides the opportunity to synthesize and consume the energetic organoazides, without accumulation thereof. In this report, we described a continuous synthesis of the antiseizure medication rufinamide. This route is convergent and features copper tubing reactor-catalyzed cycloaddition reaction. Each of the three chemical steps enjoys significant benefits and has several advantages by being conducted in flow. The total average residence time of the synthesis is approximately 11 min, and rufinamide is obtained in 92% overall yield.

 

 

 

 

 

Thumbnail image of graphical abstract

Give it a flow: A continuous-flow process for the synthesis of a 1,2,3-triazole precursor of Rufinamide has been developed. The protocol involves a solvent- and catalyst-free operation and utilizes reaction temperatures above the melting point of the target product to prevent microreactor clogging, resulting in a decrease of the operating time from hours to minutes.

Solvent- and Catalyst-Free Huisgen Cycloaddition to Rufinamide in Flow with a Greener, Less Expensive Dipolarophile

  1. Svetlana Borukhova1,
  2. Dr. Timothy Noël1,*,
  3. Bert Metten2,
  4. Eric de Vos2 and
  5. Prof. Dr. Volker Hessel1,*

Article first published online: 23 SEP 2013

DOI: 10.1002/cssc.201300684

http://onlinelibrary.wiley.com/doi/10.1002/cssc.201300684/abstract

 

 

 

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