Department of Chemistry, Indian Institute of Science Education and Research, Pune-411008, India.
Org Biomol Chem. 2018 Oct 10;16(39):7223-7229. doi: 10.1039/c8ob01852a.
Ru(ii)-NHC catalyzes α-olefination of 2-oxindoles using diaryl methanols in the absence of an acceptor. A wide array of symmetrical and unsymmetrical diaryl methanols undergoes dehydrogenative coupling with 2-oxindole selectively to generate various substituted 3-(diphenylmethylene)indolin-2-one derivatives in good yields and produces environmentally benign by-products, H2 and H2O. This methodology was successfully applied for the synthesis of a bioactive drug i.e. TAS-301. The biological activities of the synthesized 3-(diphenylmethylene)indolin-2-one derivatives were screened against the Plasmodium falciparum parasite and found to exhibit a significant activity with IC50 = 2.24 μM.
钌（II）-NHC 催化剂在没有受体的情况下，可催化二芳基甲醇对 2-氧吲哚的α-烯烃化反应。大量的对称和不对称二芳基甲醇与 2-氧吲哚选择性地进行脱氢偶联，以高产率生成各种取代的 3-（二苯基亚甲基）吲哚啉-2-酮衍生物，并产生环境友好的副产物 H2 和 H2O。该方法成功地应用于生物活性药物 TAS-301 的合成。合成的 3-（二苯基亚甲基）吲哚啉-2-酮衍生物的生物活性对恶性疟原虫寄生虫进行了筛选，发现其具有显著的活性，IC50 = 2.24 μM。
