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08월 28일 16시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능
Regioselective Benzopyranyl Pyrazole Library Construction via and Solid-Phase and Solution-Phase parallel synthesis
2008년 8월 12일 14시 12분 16초
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서울대학교 화학과, Korea
서울대학교 화학부, Korea
Collections of drug-like small molecules derived from combinatorial chemistry became essential assets for the biomedical research, especially chemical biology. The small molecule collection can be subjected to the diverse biological evaluation to identify the specific perturbagens, which can alter the individual function of gene products. These bioactive molecules can facilitate the exploration of mysterious biological pathways in cells or organism. In other word, the construction of small molecule collection with privileged substructures is the important starting point for the discovery of novel bioactive compound as a potential bioprobes or therapeutic agents. In our previous study, we demonstrated a DOS strategy to maximize the skeletal diversity based on the benzopyran-embedded heterocycles and 22 unique benzopyranyl heterocycles were synthesized in high efficiency. In addition, we extended our research campaign on the DOS pathway development toward the maximization of diversity on polar surface area with similar 3D skeleton. Therefore, we recently reported a novel divergent synthetic pathway for the construction of benzopyranyl heterocyclic series. We identify the novel reactivity and efficient transformation of s-cis-enones as versatile key intermediates toward four novel benzopyran-embedded skeletons, pyridine, pyrazole, pyrazolopyrimidine, and pyrimidine. This DOS pathway was developed to visualize the importance of the orientation and arrangement of polar surface areas on rigid core skeletons, which were designed and synthesized through a creative recombination of the privileged substructure, benzopyran. 1 In this presentation, we would like to demonstrate our current efforts on the technology adaptation of our previous pathway toward the solution-phase parallel synthesis for the construction of small molecule collection with benzopyranyl pyrazoles. We also introduced the new pending potentials for the diversity on various substituents and functional group to maximize the efficiency as well as the diversity in our final compound collection. The key point of this synthetic pathway is the regioselective synthesis of aryl and alkyl pyrazoles, which has never been reported in the literatures.
1) An, H.; Eum, S. –J.; Koh, M.; Lee, S. K.; Park, S. B., J. Org. Chem. 2008, 73, 1752.
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