Synthesis of 1-(2-(piperidin-1-yl)ethyl)-1H-pyrrole-2-carbaldehyde

1-(2-(piperidin-1-yl)ethyl)-1H-pyrrole-2-carb aldehyde 4a-b is a new aqueous solubility aldehyde as an important intermediates of small molecule anticancer drugs. In this work, a rapid synthetic method for target compounds 4a-b was established. The compound 4a-b was synthesized from the commercially available pyrrole through three steps including acylation and two steps nucleophilic substitution. The structure was confirmed by MS and 'HNMR. Furthermore, the synthetic method was optimized. The total yield of the three steps was 65%.