- Mild and efficient synthesis of carboxylic acid anhydrides from carboxylic acids and triazine coupling reagents
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Anhydrides of carboxylic acids were obtained in 53%-95% yield by treatment of appropriate carboxylic acids with 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) or 2,4-dichloro-6-methoxy-1,3,5-triazine (DCMT) in the presence of N-methylmorpholine. It has been proved that synthesis proceeds via triazine active esters 3a,b, which are able to acylate carboxylate anion but not less nucleophilic carboxylic acid.
- Kaminski, Zbigniew J.,Kolesinska, Beata,Malgorzata, Marcinkowska
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p. 3349 - 3358
(2007/10/03)
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- N-docosahexaenoyl, 3 hydroxytyramine: A dopaminergic compound that penetrates the blood-brain barrier and suppresses appetite
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Fatty acids with varying chain lengths (2-22 carbon atoms long) and degrees of unsaturation (0-6 double bonds) were used to synthesize dopaminergic compounds for a study of the carrier mediated transport of dopamine (DA) to the brain. The most active carrier was the all cis C22:6 fatty acid [docosahexaenoic acid,( DHA)]which increased DA uptake through the blood-brain barrier by greater than 7.5 fold. The DHA-DA compound, NMI 8739, depressed the general locomotor activity of mice in a dose dependent manner. It also suppressed the appetite of Balb c mice and Charles River rats by 50% and 95% respectively at a dose of 10 mg/kg. Daily administration of NMI-8739 for a three week period did not induce tolerance. These results demonstrate DHA's potential for the carrier mediated transport of small molecules to the brain.
- Shashoua, Victor E.,Hesse, Gary W.
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p. 1347 - 1357
(2007/10/03)
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