Wang Zhanguo, Yuan Yunyun, Chen Yuyan, Sun Gangchun, Wu Xianghong, Zhang Shengmei, Han Chunyan, Wang Guanxing, Li Li, Liu Gang
Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union of Medical College, 1 Xian Nong Tan Street, Beijing 100050, P. R. China.
J Comb Chem. 2007 Jul-Aug;9(4):652-60. doi: 10.1021/cc0601276. Epub 2007 May 16.
This paper discusses the synthesis of privileged structures 4H-benzo[1,4]thiazin-3-one and 1,1-dioxo-1,4-dihydro-2H-1lambda6-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 intramolecular cyclization to 1,1-dioxo-1,4-dihydro-2H-1lambda6-benzo[1,4]thiazin-3-one was achieved by microwave assistance or the use of an inorganic base.
本文讨论了以1,5-二氟-2,4-二硝基苯为原料，采用平行溶液相法合成具有特殊结构的4H-苯并[1,4]噻嗪-3-酮和1,1-二氧代-1,4-二氢-2H-1λ6-苯并[1,4]噻嗪-3-酮衍生物。每个骨架都有四个多样性位点。使用廉价高效的氧化剂尿素过氧化氢（UHP）引入砜基。通过微波辅助或使用无机碱实现分子内环化生成1,1-二氧代-1,4-二氢-2H-1λ6-苯并[1,4]噻嗪-3-酮。
