EventsThe 13th International Electronic Conference on Synthetic Organic Chemistry
Event submissions
Published
with-doi10.3390/ecsoc-13-00210
This submission belongs to the session c. Bioorganic Chemistry and Natural Products of the event The 13th International Electronic Conference on Synthetic Organic Chemistry
Published date
01 Nov, 2009
Citation
Jozef Csollei, Josef Jampilek, Radka Opatrilova, Lukas Placek, Barbora Slaba, Sylva Dittrichova, Katerina Brychtova, 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 International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2009, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-13-00210
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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

Jozef Csollei 1
Josef Jampilek 1,2
Radka Opatrilova 1
Lukas Placek 1,2
Barbora Slaba 1,2
Sylva Dittrichova 1
Katerina Brychtova 1
1. 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
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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ORGANOCATALYTIC APPROACH TO THE SYNTHESIS OF OPTICALLY ACTIVE 1,2,3-TRISUBSTITUTED AZETIDINES