EventsThe 14th International Electronic Conference on Synthetic Organic Chemistry
Event submissions
Published
with-doi10.3390/ecsoc-14-00417
This submission belongs to the session a. General Organic Synthesis of the event The 14th International Electronic Conference on Synthetic Organic Chemistry
Published date
31 Oct, 2010
Citation
Jozef Csollei, Josef Jampilek, Lukas Placek, Radka Opatrilova, Katerina Brychtova, Synthesis of Esters of 6-(2,5-Dioxopyrrolidin-1-yl)-2-(2-oxoazepan-1-yl)hexanoic Acid as Potential Transdermal Penetration Enhancers, in Proceedings of The 14th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2010, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-14-00417
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Synthesis of Esters of 6-(2,5-Dioxopyrrolidin-1-yl)-2-(2-oxoazepan-1-yl)hexanoic Acid as Potential Transdermal Penetration Enhancers

Jozef Csollei 1
Josef Jampilek 1,2
Lukas Placek 2
Radka Opatrilova 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.
2. Zentiva a.s., U kabelovny 130, 102 37 Prague 10, Czech Republic
Abstract
Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. The series of seven esters of 6-(2,5-dioxopyrrolidin-1-yl)-2-(2-oxoazepan-1-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
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