顺式-2,6-二烷基-4-氯四氢吡喃的一锅法合成及构效关系研究
One-pot synthesis and SAR study of cis-2,6-dialkyl-4-chloro-tetrahydropyrans.
作者信息
Miranda Pedro O, León Leticia G, Martín Víctor S, Padrón Juan I, Padrón José M
机构信息
Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, C/ Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
出版信息
Bioorg Med Chem Lett. 2006 Jun 15;16(12):3135-8. doi: 10.1016/j.bmcl.2006.03.064. Epub 2006 Apr 5.
A series of cis-2,6-dialkyl-4-chloro-tetrahydropyrans were prepared by means of an iron(III)-catalyzed process. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, SW1573, and WiDr. The results show that the presence of bulky substituents favors the Prins cyclization leading to new products with better activity profile against all cell lines tested.
通过铁（III）催化的方法制备了一系列顺式-2,6-二烷基-4-氯四氢吡喃。在人实体瘤细胞系A2780、SW1573和WiDr中检测了其体外抗增殖活性。结果表明，庞大取代基的存在有利于普林斯环化反应，从而产生对所有测试细胞系具有更好活性的新产物。
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