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  • 03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Solid-phase Parallel Synthesis of 2-Amino/Amido/Sulfonamido Substituted Benzo[d]oxazole Derivatives Using BAL Resin

등록일
2012년 2월 14일 19시 23분 59초
접수번호
0339
발표코드
MEDI.P-990 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 25일 (수요일) 18:00~21:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
정세린, 양정원, 양승주, 공영대
동국대학교 화학과, Korea
Heterocyclic skeletons serve as ideal scaffolds on which pharmacophores can be appended to yield potent and selective drugs. Solid-phase synthesis of combinatorial libraries has emerged as a powerful tool for efficient drug discovery process. As a part of our ongoing drug discovery program, we have been exploring the potential of resin-bound-2-amino/amido/sulfonamido substituted benzo[d]oxazole derivatives as a versatile intermediate for generation of drug-like heterocyclic compound libraries. A general method is described for the solid-phase synthesis of 2-amino/amido/sulfonamido substituted benzo[d]oxazole derivatives. The sequence developed for this purpose is based on cyclization reactions of resin-bound thioureas. N-alkylation, N-acylation and N-sulfonylation reactions of 2-amino/amido/sulfonamido substituted benzo[d]oxazole resins yield the desired variously fuctionalized benzo[d]oxazole resins. Finally, 2-amino/amido/sulfonamido substituted benzo[d]oxazole are then generated in good yields and high purities by cleavage of the respective 2-amino/amido/sulfonamido substituted benzo[d]oxazole resins. 2-amino/amido/sulfonamido substituted benzo[d]oxazole derivatives have attracted much attention for their interesting biological activities such as COX-2, 5-LO and various receptor antagonists, they serve as attractive targets for combinatorial library construction via solid-phase synthesis.

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