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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-308 |
| Subject |
Synthesis of 2-Amino-5-Carboxamide Thiazole derivatives via Dehydrative Cyclization of Thiourea Intermediate Resin on Solid Phase |
| Authors |
Ye Ji Kim, Min Jeong Cha1, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
1Dongguk University, Korea
|
| Abstract |
In this study, we synthesized 2-amino-5-carboxamide thiazole derivatives on solid phase. The synthesis of library starts from the reductive amination of the 4-formyl-3-methoxy phenoxy resin to prevent isomer formation. The dehydrative cyclization of thiourea intermediate resin, which is the key step of the synthetic process, was successfully conducted with using α-bromoketone in the presence of the dimethylformamide to afford 2-amino-5-carboxylate thiazole resin. The resulting resin undergoes amide coupling with various amines. Finally, the 2-amino-5-carboxamide thiazole resin was cleaved from the polymer support under trifluoroacetic acid in dichloromethane. Additionally, physicochemical properties of constructed 2-amino-5-carboxamide thiazole derivatives were conducted. According to the study results, the library molecules show reasonable oral bioavailability drug properties as determined by the Lipinski’s Rule. |
| E-mail |
kyj4660@hanmail.net |
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122nd General Meeting of the KCS