|
|
| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-388 |
| Subject |
Solid-Phase Synthesis of 2-Amino-5-Carboxamide Thiazole derivatives via Dehydrative Cyclization of Thiourea Intermediate Resin |
| Authors |
Ye Ji Kim, Young Dae Gong*
Department of Chemistry, Dongguk 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 synthesized using α-bromoketone in the presence of the DMF to afford 2-amino-5-carboxylate thiazole resin. Resulting resin is coupled with various amines. Finally, the 2-amino-5-carboxamide thiazole resin was cleaved from the polymer support using TFA and DCM cocktail. The physicochemical properties of proposed 2-amino-5-carboxamide thiazole derivatives were calculated which shows reasonable oral bioavailability drug properties as determined by the Lipinski’s Rule. |
| E-mail |
kyj4660@hanmail.net |
|
123rd General Meeting of the KCS