Hehua Xiong, Jia Zhi, Yingmei Zhuang
Feb 1, 2018
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Abstract
4-(4-aminophenoxy)-N-propylpicoliamide 4 is an important intermediate for the synthesis of many biologically active compounds. The compound 4-(4-aminophenoxy)-N-propylpicolinamide was obtained by three simple steps to synthesis from picolinic acid. In this paper, three novel 3-phenyl-1H-pyrazole derivatives were prepared. The structure was confirmed by MS and 1 H NMR. Furthermore, the synthetic method was optimized. The total yield of the target product was 80%. Introduction Cancer is one of the most serious diseases that threaten human life. Fast-paced life, high pressure work and disorganized lifestyle all increase our chances of getting cancer. In the same time the changing of the environment make the kinds of cancers more complex and changeable [1-3]. Traditional cancer treatment is mainly based on surgery, radiotherapy and chemotherapy. However, Most of the cancers are not obvious in the earlier stage, absolute cure is not easy for traditional therapies, and the toxic side-effect is too harmful to recover [4-5]. In recent years, with the progress of molecular biology research, molecular targeted therapy has become a hot spot as a new biological treatment method. Compared with traditional chemotherapeutic drugs, antitumor therapy designed for specific molecular target of tumor has the advantages of strong specificity, obvious curative effect and less damage to normal tissues [6-7]. 4-chloropyridine derivatives are important intermediates for many small molecule inhibitors, all of which have good pharmacokinetic activity. There are many signaling pathways in our body that affect the growth, metastasis, proliferation and proliferation of cancer cells. Small molecule inhibitors can prevent cell growth by combining with small signaling pathways and promote cell apoptosis. Part of the highly potently and selectively small molecule inhibitors are shown in Figure 1, those compounds content the fraction of 4-(4-aminophenoxy)-N-propylpicolinamide all have great curative effect. Our synthetic 4-(4-aminophenoxy)-Npropylpicolinamide 4 derivatives are an essential integral part of many similar small molecule inhibitors. There are many reported synthesis methods, most exist in shortcomings of long synthetic route, low yield, and harmful to the environment [8-9]. To solve those problems, this study designed and optimized the synthetic route and method of 4-(4-aminophenoxy) -N-propylpicolinamide derivatives. The 4-(4-aminophenoxy)-Npropylpicolinamide 4 was synthesized from 4-chloropicolinic acid main via nucleophilic substitution reaction. Make it more suitable for industrial production. 243 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)