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1-(2-(piperidin-1-yl)ethyl)-1H-pyrrole-2-carbaldehyde 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 1 HNMR. Furthermore, the synthetic method was optimized. The total yield of the three steps was 65%.

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