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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Grand Ballroom |
| Time |
10월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-309 |
| Subject |
Design and Synthesis of Novel Drug-Like 4-(1,3,4-oxadiazol-2-yl)piperazine-2,5-dione Library via Microwave Assisted Combinatorial Chemistry
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| Authors |
Si Yeon Han, Dong Jin Park1, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
1Dongguk University, Korea
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| Abstract |
We have been interested in compounds containing 2,5-piperazinedione and 1,3,4-oxadiazole due to its wide range of biological activities. In this reason, we aimed to construct 4-(1,3,4-oxadiazol-2-yl)piperazine-2,5-dione libraries. The key step in this synthetic methodology is the formation of 2,5-piperazinedione by cyclization of methyl 2-(2-(amino)acetamido)acetate. Even though several synthesis routes of 2,5-piperazinedione core skeleton derived from a reaction between N-α-chloroacetyl amino acid methyl ester and amines on solution-phase have been published, those reaction conditions generate the desired compound in low yields and require long time. Accordingly, we developed efficient route for the preparation of 2,5-piperazinedione derivatives via microwave assisted combinatorial chemistry. Microwave irradiation can reduce reaction time rapidly and give higher yields and purities compared to conventional thermal heating. So, we obtained 2,5-piperazinedione in a effective way successfully. Next, 2,5-piperazinedione intermediates are reacted with phenyl chloroformate and hydrazides in order. Finally, we can synthesize 1,3,4-oxadiazole derivatives by dehydrative cyclization. We expect that this affording library will show good therapeutic efficacy. |
| E-mail |
pywy0626@naver.com |
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122nd General Meeting of the KCS