Kinoshita Keisuke, Yamaguchi Miyuki, Sasou Hirohisa, Konishi Hideyuki, Manabe Kei
School of Pharmaceutical Sciences, University of Shizuoka.
Chem Pharm Bull (Tokyo). 2023;71(2):175-182. doi: 10.1248/cpb.c22-00809.
Palladium-catalyzed, hydroxy-group-directed C-H arylation of [1,1'-biphenyl]-2-ols with chloroarenes was performed. The reaction showed a broad substrate scope and was successfully applied to pharmaceuticals containing a chloro group. Using 2-heteroarylphenols instead of [1,1'-biphenyl]-2-ols also yielded the desired products. The arylated product was further transformed into a triphenylene derivative.
实现了钯催化、羟基导向的[1,1'-联苯]-2-醇与氯代芳烃的C-H芳基化反应。该反应具有广泛的底物范围,并成功应用于含氯基团的药物。使用2-杂芳基苯酚代替[1,1'-联苯]-2-醇也能得到所需产物。芳基化产物进一步转化为三亚苯衍生物。