Synthesis of Diethyl 2-(2-chloronicotinoyl)malonate

doi:10.2991/bst-17.2018.39

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Synthesis of Diethyl 2-(2-chloronicotinoyl)malonate

Published Feb 1, 2018 · Hehua Xiong, Yongli Duan, Shuang Jia

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Abstract

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 1 HNMR. Furthermore, the synthetic method was optimized. The total yield of the two steps was 83.3 %. Introduction As we all know, cancer become more and more complex, the traditional treatment methods such as surgery, chemotherapy and radiotherapy is not enough to treat completely. The advent of small molecule targeted inhibitors has led to a new advance in anticancer drugs. Small molecule target inhibitors mainly act on the signaling pathways involved in cancer cell growth, further hindering cell growth and promoting apoptosis [1-3]. The structure of diethyl 2-(2-chloronicotinoyl)malonate have been found in many small molecule kinase inhibitors. The structures of representative compound derivatives were shown in Fig. 1 [4-6]. Fig.1. Structure of representative 4-Chloropyridine derivatives. As have been reported, diethyl 2-(2-chloronicotinoyl)malonate derivations was an important intermediate for synthesis those active compounds. In this paper, a new 255 Copyright © 2018, the Authors. Published by Atlantis Press. This is an open access article under the CC BY-NC license (http://creativecommons.org/licenses/by-nc/4.0/). Advances in Biological Sciences Research (ABSR), volume 6 2017 2nd International Conference on Biological Sciences and Technology (BST 2017)

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This study developed a faster and more efficient method to synthesize diethyl 2-(2-chloronicotinoyl)malonate, an important intermediate in small molecule anticancer drugs, with a total yield of 83.3 %.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Synthesis of Diethyl 2-(2-chloronicotinoyl)malonate

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