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  • 05월 20일 18시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제125회 대한화학회 학술발표회 및 총회 Solid-Phase Synthesis of thiazolo[4,5-d] pyrimidine derivatives via Intramolecular Cyclization

등록일
2020년 2월 5일 15시 34분 53초
접수번호
0398
발표코드
MEDI.P-694 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
온라인 PDF 제출
발표형식
포스터
발표분야
Medicinal Chemistry
저자 및
공동저자
Su jin Lim, Dana Kim1, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
1Department of Chemistry, Sangmyung University, Korea
The fused heterocycles are one of the most attractive compounds in drug discovery field due to their various biological activities. For instance, fused pyrimidine systems have shown various biological activities such as antitumor, antiviral, etc. In this study, we were interested in the synthesis of thiazolo[4,5-d] pyrimidine derivatives via solid phase approach. There are two key reaction steps. First one, the reaction of cyanocarbonimidodithioate terminated resin and Bromoacetonitrile would provide 4-amino- thiazole-5-carbonitrile intermediate. Next, imination of the intermediate with N,N-Dimethylformamide dimethyl acetal with following treatment with various amines gives our desired thiazolo[4,5-d] pyrimidine core skeleton. Diversification is proceeded with a number of electrophiles like acyl chlorides, alkyl halides, sulfonyl chlorides. Oxidation with mCPBA and following cleavage from the resin via amines and thiols provides diverse library of thiazolo[4,5-d] pyrimidine derivatives.

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