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A solid-phase synthetic method for 3,4-dihydro-1H-2,1-benzothiazin-4-one 2,2-dioxide derivatives
- Jeon, Moon-Kook;
- Kim, Myung-Su;
- Kwon, Jeong-Jin;
- Gong, Young-Dae;
- Lee, Duck-Hyung
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22초록
Utilizing polymer-bound anthranilic acid derivatives, we were able to obtain 3,4-dihydro-1H-2,1-benzothiazine-4-one 2,2-dioxide derivatives through N-methanesulfonylation by use of sulfonyl chloride, sulfonic acid, or sodium sulfonate, N-alkylation under Mitsunobu condition, and the cyclative cleavage in 8-52% five-step overall isolated yields and 91-99% purities from Wang resin. The reactions on solid phase were monitored by on-bead ATR-FTIR spectroscopic method and checked by help of solution-phase model experiments. (C) 2008 Elsevier Ltd. All rights reserved.
키워드
combinatorial chemistry; solid-phase synthesis; benzothiazine; cyclative cleavage; DRUG DISCOVERY; SULFONIC-ACIDS; MARTINELLINE; HETEROCYCLES; LIBRARIES; STRATEGY; AGENTS; CORE; ISOXAZOLIDINES; SULFONAMIDES
- 제목
- A solid-phase synthetic method for 3,4-dihydro-1H-2,1-benzothiazin-4-one 2,2-dioxide derivatives
- 저자
- Jeon, Moon-Kook; Kim, Myung-Su; Kwon, Jeong-Jin; Gong, Young-Dae; Lee, Duck-Hyung
- 발행일
- 2008-09-15
- 유형
- Article
- 저널명
- Tetrahedron
- 권
- 64
- 호
- 38
- 페이지
- 9060 ~ 9072
- 언어
- ENG
- 출판사
- Pergamon Press Ltd.
- 발행국가
- 영국
- 분량
- 13 페이지
- ISSN
- P 0040-4020