Synthesis of Tert-butyl 4-formyl-3, 6-dihydropyridine-1(2H) -carboxylate

Abstract

Tert-butyl 4-formyl-3, 6-dihydropyridine-1(2H)-carboxylate(9) is an important intermediate for small molecule anticancer drugs. A rapid and high yield synthetic method for tert-butyl 4-formyl-3, 6-dihydropyridine-1(2H)-carboxylate was established in this work. The target compound was synthesized from the commercially available piperidin-4-ylmethanol (5) through four steps including nucleophilic substitution reaction, oxidation reaction, halogenation reaction and elimination reaction. The structure of the target product was confirmed by 1 H NMR. In addition, the synthetic method was optimized. The total yield of the four steps was high up to 71.4%. 263