Synthesis of 1-methyl-3-(5-nitropyridin-2-yl) urea

Abstract 1-methyl-3-(5-nitropyridin-2-yl) urea (8) is an important intermediate for small molecule anticancer drugs. A rapid and high yield synthetic method for 1-methyl-3-(5-nitropyridin-2-yl) urea (8) was established in this work. The target compound was synthesized from the commercially available 2-chloro-5 -nitropyridine (5) through multi-step nucleophilic reactions.The structure of the target product was confirmed by 1H NMR. In addition, the synthetic method was optimized. The total yield of the four steps was high up to 92%.