Nickel-Catalyzed 8-Endo Cyclization/Carbonylation for the Synthesis of Eight-Membered Lactams
Yibin He1, Zilin Huang1, Yuting Jiang1
1School of Chemistry and Chemical Engineering, Key Laboratory of Surface & Interface Science of Polymer Materials of Zhejiang Province, Zhejiang Sci-Tech University, Hangzhou, Zhejiang 310018, People's Republic of China.
Abstract:
Medium-sized lactams are prevalent motifs in many bioactive molecules and natural products. However, their construction remains challenging due to unfavorable enthalpic and entropic barriers during the transition state. Herein, a novel nickel-catalyzed 8-endo cyclization/carbonylation has been achieved for the synthesis of eight-membered lactams bearing a gem-difluoro group. This approach features high regioselectivity, good functional group tolerance, and CO gas-free operation, which provides a good supplement for the preparation of eight-membered lactams via a nickel-catalyzed carbonylation process.
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