The Synaptic Leap

 

 
The next step in the PZQ synthesis via the Pictet-Spengler route is an aminoalkylation of the chloroacetamide 2 with aminoacetaldehyde dimethyl acetal 3. The aminoacetal also acted as a base to trap the HCl which was generated during the reaction and therefore 2.1 equivalents were used. The aminoacetal could be easily recovered by basic liberation of its HCl-salt which precipitated from the cold toluene solution. The crude product was obtained as a brown oil and was isolated by forming the HCl-salt 4 in an overall yield of 79%. (lit.[1] 67%)
 

Can we publish papers based on data that have previously been made public? Is a conference presentation prior disclosure? If we worked together to write a review article on a wiki, can we submit it for publication? If we conduct an open source research project with a number of collaborators on a website, where can we send the resulting articles for peer-review?

These issues are important. It is difficult to recommend conducting open research to students if they cannot be sure to get peer-reviewed papers out of their research.

The policies of many journals are out of date on these issues, owing to the enormous advances in web technologies over the last few years. To clarify such policies, a few of us have assembled a draft letter we intend to send to publishers.

Dear all,

As of today, a place has been created over at FriendFeed (FF). dedicated to Open Notebook Science.

LINK

Since this of relevance to TSL, I thought folks here might be interested to know this.

As such, this is the first link between TSL and FF that I am aware of.

Kind regards,

Graham 

Source:-

http://blog.openmedicine.ca/node/104

On October 22nd, 2007 Open Medicine will
join more than 230 scientific journals from around the world to publish
articles devoted to global health. Some of the most important health
issues that we are facing globally include the implications
of war and civil unrest, the spread of HIV/AIDS, infectious disease,
physician brain drain from developing countries, climate change and
children's/ women's health.

C'est possible que tout le monde sait que la quinine est employé contre la malaria.

Cependant, j'avais lu d'un traitement différent. Un traitement également vieux -- c'est bleu de méthylène.

Il serait certainement peu coûteux comparé à la plupart des autres traitements. Même si il n'est pas très efficace, serait-il meilleur qu'aucun traitement du tout, n'est-ce-pas ?

Savez-vous . . . ce qui s'est produit avec l'idée du bleu de méthylène ?

Je sais que c'est éteint de la voie génétique-metabolomic-enzymatique, mais parfois le remède le plus simple est le seul qui fonctionnera réellement. Remercie beaucoup.

On a proposé Hydroxyurea comme traitement possible pour la toxoplasmose.

À cet effet, j'avais essayer trouver quelquechose qu'on pourrait employer -- ou qu'un docteur, s'occupant des patients sans les ressources financières, pourrait employer, au lieu des drogues indisponibles de prescription.

J'ai trouvé une usine. L'herbe « romarin » Rosmarinus officinalis).

Alors . . . combien de fois l'agneau c'est servi rare?  Il semble, toujours.  Avec de la sauce à romarin.

C'est un antidote immédiat?  Que pensez-vous?

Hydroxyurea is a possible treatment for toxoplasmosis:

FEMS Microbiol Lett. 2000 Apr 1;185(1):79-82. Hydroxyurea inhibits intracellular Toxoplasma gondii multiplication. de Melo EJ, Mayerhoffer RO, de Souza W.

With this in mind, I went looking to see if there were anything that an average person might use -- or that a doctor, caring for patients with no financial resources, might use, in lieu of unavailable prescription drugs.

One thing did turn up.  Rosemary, the herb, the plant (Rosmarinus officinalis L. - Lamiaceae).  It contains 3-BETA-HYDROXYUREA-12,20(30)-DIEN-17-ON-ACID. 

     I've been following and participating in the Open Science community for a while now.  It's ironic, but I suffer from the same tendencies that Ginger (synapticleap.org founder) mentions in the most recent discussion "If you build it will they come".  I too have emailed with praise of her efforts, but did not post.  I'm not nearly as accomplished a scientist as some of the participants here, but do realize every effort counts.  However, still I did not post.  So this is my first post with some my observations about Open Science.

Is anyone engaged in providing Artemesia annua (artemesia) plants or seeds, to malaria-ridden areas? 

Could residents grow their own plants and either grind the leaves, or steep them into tea, etc. - in order to make their own herbal medicine?

Waiting for tablets and capsules from the Western world may take a long time, and be very expensive.

We have a problem in synthesizing our anti-malarials that could use some feedback from some organic chemists:

Ever since we isolated our Ugi products, we've been trying to cyclize them to the diketopiperazines. As described by Hulme, we are trying to effect an intramolecular transamidation catalyzed by trifluoroacetic acid (TFA). Instead of dichloroethane we are generally using CDCl3 so that we can monitor the reaction by NMR.

The first step of removing the boc group seems to proceed very smoothly, with the appearance of t-butyl trifluoroacetate at 1.61 ppm within a few minutes or hours, depending on the concentration of TFA. Here is a H NMR from Khalid's EXP070, 13 min after addition of 50% TFA in CDCl3 showing complete deprotection: