Parallel Solution-Phase Synthesis of 4H-Benzo[1,4]thiazin-3-one and 1,1-Dioxo-1,4-dihydro-2H-16-benzo[1,4]thiazin-3-one
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- 作者：Zhanguo Wang ; Yunyun Yuan ; Yuyan Chen ; Gangchun Sun ; Xianghong Wu ; Shengmei Zhang ; Chunyan Han ; Guanxing Wang ; Li Li ; Gang Liu
- 刊名：Journal of Combinatorial Chemistry
- 出版年：2007
- 出版时间：July 2007
- 年：2007
- 卷：9
- 期：4
- 页码：652 - 660
- 全文大小：171K
- 年卷期：v.9,no.4(July 2007)
- ISSN：1520-4774
文摘
This paper discusses the synthesis of privileged structures 4H-benzo[1,4]thiazin-3-one and 1,1-dioxo-1,4-dihydro-2H-1
6-benzo[1,4]thiazin-3-one derivatives in a parallel solution-phase manner using 1,5-difluoro-2,4-dinitrobenzene. Each scaffold possesses four diversity points. A cheap and efficient oxidant,urea-hydrogen peroxide (UHP), was applied for the introduction of the sulfone group. The intramolecularcyclization to 1,1-dioxo-1,4-dihydro-2H-16-benzo[1,4]thiazin-3-one was achieved by microwave assistanceor the use of an inorganic base.
6-benzo[1,4]thiazin-3-one derivatives in a parallel solution-phase manner using 1,5-difluoro-2,4-dinitrobenzene. Each scaffold possesses four diversity points. A cheap and efficient oxidant,urea-hydrogen peroxide (UHP), was applied for the introduction of the sulfone group. The intramolecularcyclization to 1,1-dioxo-1,4-dihydro-2H-16-benzo[1,4]thiazin-3-one was achieved by microwave assistanceor the use of an inorganic base.