Synthesis of Diethyl 2-(2-chloronicotinoyl)malonate

摘要

Diethyl 2-(2-chloronicotinoyl)malonate 3 is a nitrogen-containing water-soluble carboxylic acid as an important intermediates of small molecule anticancer drugs. In this study, this paper explored a faster and celerity method to synthesize compound 3. By using 2-chloronicotinic acid as a kind of easily available compound through two steps to made the target compound. The structure was confirmed by MS and ~1HNMR. Furthermore, the synthetic method was optimized. The total yield of the two steps was 83.3%.