Department of Pharmacognosy, School of Pharmacy, The University of Mississippi, University, Mississippi 38677, United States.
J Org Chem. 2012 May 18;77(10):4578-85. doi: 10.1021/jo300303d. Epub 2012 Apr 30.
A simple, mild, cost-effective, and green approach for the reductive mono-N-alkylation of nitroarenes has been developed. HOAc/Zn are utilized as the reducing system together with a carbonyl compound as an alkyl source in methanol. Excellent yields were obtained with stoichiometric control of mono- over dialkylated products. Application to five complex natural products demonstrated the practical utility of the method.
一种简单、温和、经济且环保的方法被开发出来，用于还原单 N-烷基化硝基芳烃。HOAc/Zn 被用作还原体系，同时在甲醇中利用羰基化合物作为烷基源。通过使用化学计量控制，单烷基化产物的产率非常高，而二烷基化产物的产率则较低。该方法应用于五种复杂的天然产物，展示了其实用性。
