Radical C(sp<sup>2</sup>)–H Trifluoromethylation of Aldehydes in Aqueous Solution
作者:Pei Zhang、Haigen Shen、Lin Zhu、Weiguo Cao、Chaozhong Li
DOI:10.1021/acs.orglett.8b03012
日期:2018.11.16
The copper-mediated C(sp2)–H trifluoromethylation of aldehydes is described. The reaction of aldehydes with (bpy)Cu(CF3)3, Et3SiH, and K2S2O8 in aqueous acetone at room temperature provides the corresponding trifluoromethyl ketones in satisfactory yields. The protocol is applicable to both aliphatic and aromatic aldehydes and exhibits a broad substrate scope and wide functional group compatibility
描述了铜介导的醛的C(sp 2)–H三氟甲基化。在室温下,醛与(bpy)Cu(CF 3)3,Et 3 SiH和K 2 S 2 O 8在丙酮水溶液中的反应以令人满意的产率提供了相应的三氟甲基酮。该协议适用于脂族和芳族醛,并具有广泛的底物范围和广泛的官能团相容性。提出了一种涉及Cu(II)介导的酰基三氟甲基化的机理。
Base-Mediated Cyclocondensation of Salicylaldehydes and 2-Bromoallyl Sulfones for the Synthesis of 3-Sulfonylchromene Derivatives and Their Regioselective Friedel–Crafts Heteroarylation Reactions
作者:Anand Kumar、Srinivas Thadkapally、Rajeev S. Menon
DOI:10.1021/acs.joc.5b02324
日期:2015.11.6
Cesium carbonate-mediated reaction of 2-hydroxybenzaldehydes and 2-bromoallyl sulfones afforded 2H- and 4H-chromenol derivatives endowed with a 3-arylsulfonyl group. 2-Bromoallyl sulfones functioned as synthetic equivalents of allenyl sulfones under these conditions. The 2H- and 4H-chromenol derivatives underwent regioselectiveFriedel–Craftsreactions with heteroarenes in the presence of p-toluenesulfonic
由碳酸铯介导的2-羟基苯甲醛和2-溴烯丙基砜的反应,得到具有3-芳基磺酰基的2 H-和4 H-苯甲醇衍生物。在这些条件下,2-溴烯丙基砜起着烯丙基砜的合成等同物的作用。在对甲苯磺酸的存在下,2 H-和4 H- chromenol衍生物与杂芳烃进行区域选择性Friedel-Crafts反应,以优异的收率得到4-杂芳基-4 H - chromene衍生物。
Metalloproteinase inhibitor compounds
申请人:Barlaam B. Christophe
公开号:US20060287338A1
公开(公告)日:2006-12-21
Compounds of the formula I
useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.