Division of Organic Chemistry, CSIR-National Chemical Laboratory , Pune 411 008, India.
J Org Chem. 2017 Jun 16;82(12):6366-6372. doi: 10.1021/acs.joc.7b00948. Epub 2017 May 24.
The Pd-catalyzed quinazolinone-directed regioselective monoarylation of aromatic rings by C-H bond activation is developed. A broad substrate scope is demonstrated for both quinazolinone as well as diaryliodonium triflates. The use of a base was found to be crucial for this transformation, unlike for the known nitrogen-directed arylations. All of the novel quinazolinones of biological interest were synthesized by using the operationally simple Pd(II)-catalyzed arylation reaction.
Pd 催化的喹唑啉酮导向的芳环 C-H 键活化区域选择性单芳基化反应得到发展。该反应对喹唑啉酮和二芳基碘鎓三氟甲磺酸酯都具有广泛的底物适用性。与已知的氮导向芳基化反应不同，该转化需要使用碱。所有具有生物活性的新型喹唑啉酮都是通过操作简单的 Pd(II)催化的芳基化反应合成的。
