A solid-phase synthetic method for 3,4-dihydro-1H-2,1-benzothiazin-4-one 2,2-dioxide derivatives |
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Authors: | Moon-Kook Jeon Myung-Su Kim Jeong-Jin Kwon Young-Dae Gong |
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Affiliation: | a Korea Research Institute of Chemical Technology, PO Box 107, Yuseong-gu, Daejeon 305-600, Republic of Korea b Department of Chemistry, Sogang University, Seoul 151-742, Republic of Korea |
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Abstract: | 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. |
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Keywords: | Combinatorial chemistry Solid-phase synthesis Benzothiazine Cyclative cleavage |
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