Resolution of Praziquantel
Publication Date
September 20, 2011
Journal
PLOS Neglected Tropical Diseases
Authors
Michael Woelfle, Jean Paul Seerden, Jesse De Gooijer, Kees Pouwer, et al
Volume
5
Issue
9
Pages
e1260
DOI
https://dx.plos.org/10.1371/journal.pntd.0001260
Publisher URL
http://journals.plos.org/plosntds/article?id=10.1371%2Fjournal.pntd.0001260
PubMed
http://www.ncbi.nlm.nih.gov/pubmed/21949890
PubMed Central
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3176743
Europe PMC
http://europepmc.org/abstract/MED/21949890
Web of Science
000296578900005
Scopus
80053458170
Mendeley
http://www.mendeley.com/research/resolution-praziquantel
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Mendeley | Further Information

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CrossRef

Scopus | Further Information

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Figshare

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  • {"files"=>["https://ndownloader.figshare.com/files/733017"], "description"=>"<p>General approaches to the preparation of enantiopure praziquantel (PZQ).</p>", "links"=>[], "tags"=>["approaches", "enantiopure", "praziquantel"], "article_id"=>403372, "categories"=>["Chemistry", "Infectious Diseases"], "users"=>["Michael Woelfle", "Jean-Paul Seerden", "Jesse de Gooijer", "Kees Pouwer", "Piero Olliaro", "Matthew H. Todd"], "doi"=>"https://dx.doi.org/10.1371/journal.pntd.0001260.g001", "stats"=>{"downloads"=>3, "page_views"=>16, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/_General_approaches_to_the_preparation_of_enantiopure_praziquantel_PZQ_/403372", "title"=>"General approaches to the preparation of enantiopure praziquantel (PZQ).", "pos_in_sequence"=>0, "defined_type"=>1, "published_date"=>"2011-09-20 00:56:12"}
  • {"files"=>["https://ndownloader.figshare.com/files/370337", "https://ndownloader.figshare.com/files/370364", "https://ndownloader.figshare.com/files/370400", "https://ndownloader.figshare.com/files/370470", "https://ndownloader.figshare.com/files/370523", "https://ndownloader.figshare.com/files/370554", "https://ndownloader.figshare.com/files/370576", "https://ndownloader.figshare.com/files/370619", "https://ndownloader.figshare.com/files/370656", "https://ndownloader.figshare.com/files/370697", "https://ndownloader.figshare.com/files/370734", "https://ndownloader.figshare.com/files/370753", "https://ndownloader.figshare.com/files/370784", "https://ndownloader.figshare.com/files/370820", "https://ndownloader.figshare.com/files/371010"], "description"=>"<div><h3>Background</h3><p>Praziquantel remains the drug of choice for the worldwide treatment and control of schistosomiasis. The drug is synthesized and administered as a racemate. Use of the pure active enantiomer would be desirable since the inactive enantiomer is associated with side effects and is responsible for the extremely bitter taste of the pill.</p> <h3>Methodology/Principal Findings</h3><p>We have identified two resolution approaches toward the production of praziquantel as a single enantiomer. One approach starts with commercially available praziquantel and involves a hydrolysis to an intermediate amine, which is resolved with a derivative of tartaric acid. This method was discovered through an open collaboration on the internet. The second method, identified by a contract research organisation, employs a different intermediate that may be resolved with tartaric acid itself.</p> <h3>Conclusions/Significance</h3><p>Both resolution procedures identified show promise for the large-scale, economically viable production of praziquantel as a single enantiomer for a low price. Additionally, they may be employed by laboratories for the production of smaller amounts of enantiopure drug for research purposes that should be useful in, for example, elucidation of the drug's mechanism of action.</p> </div>", "links"=>[], "tags"=>["praziquantel"], "article_id"=>133166, "categories"=>["Cancer", "Chemistry"], "users"=>["Michael Woelfle", "Jean-Paul Seerden", "Jesse de Gooijer", "Kees Pouwer", "Piero Olliaro", "Matthew H. Todd"], "doi"=>["https://dx.doi.org/10.1371/journal.pntd.0001260.s001", "https://dx.doi.org/10.1371/journal.pntd.0001260.s002", "https://dx.doi.org/10.1371/journal.pntd.0001260.s003", "https://dx.doi.org/10.1371/journal.pntd.0001260.s004", "https://dx.doi.org/10.1371/journal.pntd.0001260.s005", "https://dx.doi.org/10.1371/journal.pntd.0001260.s006", "https://dx.doi.org/10.1371/journal.pntd.0001260.s007", "https://dx.doi.org/10.1371/journal.pntd.0001260.s008", "https://dx.doi.org/10.1371/journal.pntd.0001260.s009", "https://dx.doi.org/10.1371/journal.pntd.0001260.s010", "https://dx.doi.org/10.1371/journal.pntd.0001260.s011", "https://dx.doi.org/10.1371/journal.pntd.0001260.s012", "https://dx.doi.org/10.1371/journal.pntd.0001260.s013", "https://dx.doi.org/10.1371/journal.pntd.0001260.s014", "https://dx.doi.org/10.1371/journal.pntd.0001260.s015"], "stats"=>{"downloads"=>26, "page_views"=>13, "likes"=>0}, "figshare_url"=>"https://figshare.com/articles/Resolution_of_Praziquantel/133166", "title"=>"Resolution of Praziquantel", "pos_in_sequence"=>0, "defined_type"=>4, "published_date"=>"2011-09-20 00:52:46"}

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Relative Metric

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