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Usage Statistics Cite this paper as: Brychtova, K.; Dittrichova, S.; Slaba, B.; Placek, L.; Opatrilova, R.; Jampilek, J.; Csollei, J. Synthesis of Esters of 6-(2,5-Dioxopyrrolidin-1-yl)-2- (morpholin-4-yl)hexanoic Acid as Potential Transdermal Penetration Enhancers. In Proceedings of the 13th Int. Electron. Conf. Synth. Org. Chem., 1-30 November 2009; Sciforum Electronic Conferences Series, 2009, c010:1-6.
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13th Int. Electron. Conf. Synth. Org. Chem. 2009, c010:1-6
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Synthesis of Esters of 6-(2,5-Dioxopyrrolidin-1-yl)-2- (morpholin-4-yl)hexanoic Acid as Potential Transdermal Penetration Enhancers
Katerina Brychtova 1,* 
, Sylva Dittrichova 1, Barbora Slaba 1,2, Lukas Placek 1,2, Radka Opatrilova 1, Josef Jampilek 1,2 and Jozef Csollei 1
, Sylva Dittrichova 1, Barbora Slaba 1,2, Lukas Placek 1,2, Radka Opatrilova 1, Josef Jampilek 1,2 and Jozef Csollei 11 Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic; e-mail: brychtovak@vfu.cz, tel: +420-5-41562924;
2 Zentiva a.s., U kabelovny 130, 102 37 Prague 10, Czech Republic;
* Author to whom correspondence should be addressed.
(This article belongs to the section C. Bioorganic Chemistry and Natural Products)
Abstract: Skin penetration enhancers are used to allow formulation of transdermal delivery systems for drugs that are otherwise insufficiently skin-permeable. The series of seven esters of 6-(2,5-dioxopyrrolidin-1-yl)-2-(morpholin-4-yl)hexanoic acid as potential transdermal penetration enhancers was formed by multistep synthesis. The general synthetic approach of all newly synthesized compounds is presented. Structure confirmation of all generated compounds was accomplished by IR, 1H, 13C NMR and HR-MS spectroscopy. All the prepared compounds were analyzed using RP-HPLC method for the lipophilicity measurement and their lipophilicity (log k) was determined.
Keywords: Transdermal penetration enhancers; 6-Aminohexanoic acid derivatives; Lipophilicity
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