Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole
The research and development of effective anti-cancer drugs have been urgently needed. Molecular targeted drugs can be used to target tumor cells, which have good curative effect and little adverse reactions, and gradually become the development direction of anti-tumor drugs. As a molecular target d...
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doaj-cc7ae9a1f70a401aa6c74da9d980958d2020-12-17T07:36:25ZzhoEditorial Board of Journal of IsotopesJournal of Isotopes1000-75121000-75122020-12-0133624124710.7538/tws.2017.youxian.071Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]TriazoleXU Zhongjie1,2;TU Yahui1,2;ZHONG Jiaqi1,2;SUN Wen1,2;WANG Zhonghua3;WANG Haoran1,2;BAI Shaofei1,2;WU Fanhong301.National Isotope Engineering Technology Research CenterShanghai Sub-Center, Shanghai Research Institute of Chemical Industry CO. LTD., Shanghai 200062, China; 2.Shanghai Engineering Research Center of Stable Isotope, Shanghai Research Institute of Chemical Industry CO. LTD., Shanghai 200062, China; 3.Shanghai Institute of Technology, Shanghai 201418, ChinaThe research and development of effective anti-cancer drugs have been urgently needed. Molecular targeted drugs can be used to target tumor cells, which have good curative effect and little adverse reactions, and gradually become the development direction of anti-tumor drugs. As a molecular target drug Combretastatin A4 (CA4) can inhibit tubulin polymerization and splitso that researchers pay more and more attention to the modification of CA4 structure and similar things. The development of this area becomes one of the direction of anti-tumor drugs research hot spot. This article presented an efficient synthesis method of 1-(3-methoxy-phenyl)-[4-(4-Fluoro-2-methoxy-D3-phenylaminemethyl]-1H-[1,2,3]triazole with iodomethane-D3 as the common substrate, which was mainly obtained through methylation, reduction, substitution,azidation and cyclization reaction. The yields of 1-(3-methoxy-phenyl)-[4-(4-Fluoro-2-methoxy-D3-phenylaminemethyl]-1H-[1,2,3]triazole was 60.2% based on iodomethane-D3 consumed. The chemical purity of this product was 99.0% and deuterium isotopic enrichment of this product was 99.0%. The compound could be used in the field of antitumor drug because of a broad range of anticancer activity of it.http://www.tws.org.cn/CN/abstract/abstract1827.shtmlcombretastatin a4 stable isotope anti-tumor activity |
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zho |
format |
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DOAJ |
author |
XU Zhongjie1,2;TU Yahui1,2;ZHONG Jiaqi1,2;SUN Wen1,2;WANG Zhonghua3;WANG Haoran1,2;BAI Shaofei1,2;WU Fanhong3 |
spellingShingle |
XU Zhongjie1,2;TU Yahui1,2;ZHONG Jiaqi1,2;SUN Wen1,2;WANG Zhonghua3;WANG Haoran1,2;BAI Shaofei1,2;WU Fanhong3 Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole Journal of Isotopes combretastatin a4 stable isotope anti-tumor activity |
author_facet |
XU Zhongjie1,2;TU Yahui1,2;ZHONG Jiaqi1,2;SUN Wen1,2;WANG Zhonghua3;WANG Haoran1,2;BAI Shaofei1,2;WU Fanhong3 |
author_sort |
XU Zhongjie1,2;TU Yahui1,2;ZHONG Jiaqi1,2;SUN Wen1,2;WANG Zhonghua3;WANG Haoran1,2;BAI Shaofei1,2;WU Fanhong3 |
title |
Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole |
title_short |
Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole |
title_full |
Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole |
title_fullStr |
Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole |
title_full_unstemmed |
Syntheses of Stable Isotopelabeled 1-(3-Methoxy-Phenyl)-[4-(4-Fluoro-2-Methoxy-D3-Phenylaminemethyl]-1h-[1,2,3]Triazole |
title_sort |
syntheses of stable isotopelabeled 1-(3-methoxy-phenyl)-[4-(4-fluoro-2-methoxy-d3-phenylaminemethyl]-1h-[1,2,3]triazole |
publisher |
Editorial Board of Journal of Isotopes |
series |
Journal of Isotopes |
issn |
1000-7512 1000-7512 |
publishDate |
2020-12-01 |
description |
The research and development of effective anti-cancer drugs have been urgently needed. Molecular targeted drugs can be used to target tumor cells, which have good curative effect and little adverse reactions, and gradually become the development direction of anti-tumor drugs. As a molecular target drug Combretastatin A4 (CA4) can inhibit tubulin polymerization and splitso that researchers pay more and more attention to the modification of CA4 structure and similar things. The development of this area becomes one of the direction of anti-tumor drugs research hot spot. This article presented an efficient synthesis method of 1-(3-methoxy-phenyl)-[4-(4-Fluoro-2-methoxy-D3-phenylaminemethyl]-1H-[1,2,3]triazole with iodomethane-D3 as the common substrate, which was mainly obtained through methylation, reduction, substitution,azidation and cyclization reaction. The yields of 1-(3-methoxy-phenyl)-[4-(4-Fluoro-2-methoxy-D3-phenylaminemethyl]-1H-[1,2,3]triazole was 60.2% based on iodomethane-D3 consumed. The chemical purity of this product was 99.0% and deuterium isotopic enrichment of this product was 99.0%. The compound could be used in the field of antitumor drug because of a broad range of anticancer activity of it. |
topic |
combretastatin a4 stable isotope anti-tumor activity |
url |
http://www.tws.org.cn/CN/abstract/abstract1827.shtml |
work_keys_str_mv |
AT xuzhongjie12tuyahui12zhongjiaqi12sunwen12wangzhonghua3wanghaoran12baishaofei12wufanhong3 synthesesofstableisotopelabeled13methoxyphenyl44fluoro2methoxyd3phenylaminemethyl1h123triazole |
_version_ |
1724380004836442112 |