State Key Laboratory of Natural Medicines (SKLNM) and Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University , Nanjing 210009, China.
Org Lett. 2017 Jun 2;19(11):2829-2832. doi: 10.1021/acs.orglett.7b00930. Epub 2017 May 16.
A Rh-catalyzed enol-directed formal sp C-H activation/annulation of α-arylidene pyrazolones with alkynes has been developed. This reaction provides a convenient route to synthesize spiropentadiene pyrazolones in good to excellent yields at room temperature, exhibiting good functional group tolerance, gram scalability, and high regioselectivity. Of note, the α-arylidene pyrazolone was introduced as a novel C3 synthon in C-H activation/annulation.
发展了一种 Rh 催化的烯醇导向的α-芳亚甲基吡唑酮的形式 sp³ C-H 活化/环化反应与炔烃。该反应在室温下以良好至优秀的收率提供了一种方便的合成螺戊二烯吡唑酮的方法，具有良好的官能团耐受性、克级规模和高区域选择性。值得注意的是，α-芳亚甲基吡唑酮被引入到 C-H 活化/环化反应中作为一种新型的 C3 合成子。
