Synthesis and pharmacology of centrally acting dopamine derivatives and analogs in relation to Parkinson's disease

Solid Lipid Microparticles for the Stability Enhancement of a Dopamine Prodrug

“…11,12 In order to verify the ability of DVD to be hydrolyzed into dopamine in physiologic environments (or in other word to verify if it can be its prodrug) we have analyzed its stability in human plasma by a new HPLC method. Assay validation indicated that the chromatographic precision for the prodrug DVD and its internal standard (PTP) was represented by RSD values of 1.48%, 1.86%, and 2.32% for 100 mM DVD, 10 mM DVD, and 10 mM internal standard, respectively.…”

Simultaneous quantitative analysis of methamphetamine and 4-hydroxymethamphetamine in body fluids by gas chromatography/mass spectrometry

“…4-Hydroxyamphetamine(HAMP) hydrobromide (m.p. 195°-196°C) was prepared by heating 4-methoxyamphetamine [5] in 47% HBr at 125°C and recrystallization from isopropanol-diethyl ether [6]. 4-Hydroxymethamphetamine (m.p.…”

“…The ether dehydrated with potassium carbonate was transferred to a flask and condensed in a water bath at 50°C. Next, 6ml benzaldehyde was poured into the flask, and the preparation was heated in a boiling water bath for 2 h. A Schiff base of the primary amine and benzaldehyde was formed [6,7]. The base was mixed with 6 ml dimethyl-d6 sulfate in 20 ml of benzene and heated in a steam bath for 1 h. The resulting salt was extracted into 30 ml of distilled water.…”

The Development of a Convergent and Efficient Enantioselective Synthesis of the Bengamides via a Common Polyol Intermediate

“…Hydrolysis of the imino function of 43 was effected with 10% aqueous citric acid/THF 1 : 1 [28], and debenzylation by hydrogenation (1 atm) over 5 mol-% of Pearlman×s catalyst in EtOH [29], affording 44 in 86% overall yield. Treatment of 44 with MeONa in MeOH at 858 (sealed tube) [32]. The selective O-acylation was achieved by irreversible protonation of the a-amino group in the strongly acidic medium [32].…”

“…Treatment of 44 with MeONa in MeOH at 858 (sealed tube) [32]. The selective O-acylation was achieved by irreversible protonation of the a-amino group in the strongly acidic medium [32]. The synthetic route presented to the lactam subunits 46 and 47 features several noteworthy elements: 1) complete stereoselectivity and high overall yield, requiring purification at only three stages (37, 43, and 46 or 47); 2) the possibility for structural variation at several stages, e.g., through the use of different bifunctional electrophiles (instead of 10) or alkyl groups on the lactam N-atom and the acyl group on the secondary alcohol; and 3) the economy of our method, which is based on inexpensive starting materials and reagents.…”