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Improved Synthesis of Dbibb as a New Anti-Radiation Agent

Improved Synthesis of Dbibb as a New Anti-Radiation Agent An excellent candidate in the fight against damage caused by nuclear radiation is 2-[4-(1,3-dioxo-1H,3Hbenzoisoquinolin-2-yl)butylsulfamoyl]benzoic acid (DBIBB), a lipid agonist of lysophospholipid acid receptor 2. In this study, a novel method that synthesizes DBIBB was developed. In this method, saccharin was replaced singly by 1,4-dibromobutane, reacted with 1,8-naphthalimide, hydrolyzed by sodium hydroxide, and finally acidified by hydrochloric acid to obtain DBIBB. The new synthesis route was shorter, milder, and simpler than previously reported approaches. The method also produced higher total yield than that of existing ones. Thus, it is applicable to the large-scale synthesis of DBIBB. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Chemistry of Natural Compounds Springer Journals

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Publisher
Springer Journals
Copyright
Copyright © 2018 by Springer Science+Business Media, LLC, part of Springer Nature
Subject
Pharmacy; Pharmacy; Organic Chemistry; Plant Sciences
ISSN
0009-3130
eISSN
1573-8388
DOI
10.1007/s10600-018-2388-x
Publisher site
See Article on Publisher Site

Abstract

An excellent candidate in the fight against damage caused by nuclear radiation is 2-[4-(1,3-dioxo-1H,3Hbenzoisoquinolin-2-yl)butylsulfamoyl]benzoic acid (DBIBB), a lipid agonist of lysophospholipid acid receptor 2. In this study, a novel method that synthesizes DBIBB was developed. In this method, saccharin was replaced singly by 1,4-dibromobutane, reacted with 1,8-naphthalimide, hydrolyzed by sodium hydroxide, and finally acidified by hydrochloric acid to obtain DBIBB. The new synthesis route was shorter, milder, and simpler than previously reported approaches. The method also produced higher total yield than that of existing ones. Thus, it is applicable to the large-scale synthesis of DBIBB.

Journal

Chemistry of Natural CompoundsSpringer Journals

Published: Jun 7, 2018

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