Synthesis of 4-(pyrrolidin-1-ylmethyl)benzaldehyde

Abstract

4-(pyrrolidin-1-ylmethyl)benzaldehyde (1) as a water-soluble aldehyde is an important intermediate for small molecule anticancer drugs. A rapid and high yield synthetic method for 4-(pyrrolidin-1-ylmethyl)benzaldehyde (1) was established in this work. The target compound was synthesized from the commercially available terephthalaldehyde (6) through three steps including acetal reaction, nucleophilic reaction and hydrolysis reaction. The structure of the target product was confirmed by 1 H NMR and MS. In addition, the synthetic method was optimized. The total yield of the three steps was high up to 68.9%.