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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-390 |
| Subject |
Design and Solid-Phase Parallel Synthesis of 2,4,5-Trisubstituted Thiazole Derivatives via Cyclization Reaction with a Carbamimidothioate Linker |
| Authors |
Hyejin Kwon, Hyungha Park, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
|
| Abstract |
Preparation of 2,4,5-trisubstituted thiazole derivatives via a new solid-phase synthetic route has been conducted in this study. The synthetic route begins with synthesis of a core skeleton 2,4-diamino(thiazole-5-yl)substituted-phenylmethanone resin, obtained through a cyclization reaction with a carbamimidothioate linker. The core skeleton was substituted with diverse building blocks such as amines, alkyl halides, and acid chlorides. The products were cleaved from the solid support via TFA/CH2Cl cleavage cocktail. Overall, the strategy permits the incorporation of three points of diversity into the thiazole ring system with good overall yields.1 Finally, 2,4,5-trisubstituted thiazole derivatives library showed oral bioavailability through calculation of the physicochemical properties. |
| E-mail |
khgin@hanmail.net |
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123rd General Meeting of the KCS