首页> 外国专利> METHOD FOR PREPARING BENZOFURAN COMPOUNDS INCLUDING GRAMNIPHENOL F, GRAMNIPHENOL G, CICERFURAN, MORUNIGROL C AND DERIVATIVES THEREOF

METHOD FOR PREPARING BENZOFURAN COMPOUNDS INCLUDING GRAMNIPHENOL F, GRAMNIPHENOL G, CICERFURAN, MORUNIGROL C AND DERIVATIVES THEREOF

机译:苯并呋喃化合物的制备方法,包括苯丙酚F,苯丙酚G,西塞呋喃,莫瑞洛尔C及其衍生物

摘要

The present invention relates to a method for preparing natural benzofurans including gramniphenol F, gramniphenol G, morunigrol C and 3′,5′-di-O-methyl analogues thereof and cicerfuran by using 2,4-dihydroxybenzaldehyde, 5-bromoresorcinol and sesamol. In the method according to the present invention, region-selective prenylation, Ramirez gem-dibromo olefination, Miyaura borylation and Suzuki coupling are used. In addition, the compounds were determined for anti-inflammatory effects through a test for production of nitrogen oxide in liposaccharide-induced RAW-264.7 macrophages. All of the compounds show weak to medium (16-42%) inhibitory activities, are not toxic and have an IC_50 value of 9.1 to 25.2 μM.;COPYRIGHT KIPO 2017
机译:本发明涉及一种通过使用2,4-二羟基苯甲醛,5-溴代间苯二酚和芝麻酚来制备天然苯并呋喃的方法,所述天然苯并呋喃包括萘酚F,萘酚G,莫瑞戈尔C及其3-,-,5--二-O-甲基类似物和环呋喃。在根据本发明的方法中,使用区域选择性的烯丙基化,拉米雷斯宝石-二溴烯烃化,宫浦硼酸化和铃木偶联。此外,通过测试脂糖诱导的RAW-264.7巨噬细胞中一氧化氮的产生来确定化合物的抗炎作用。所有化合物均显示弱至中度​​(16-42%)抑制活性,无毒且IC_50值为9.1至25.2μM。; COPYRIGHT KIPO 2017

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