Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Solvent Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines

Version 1 : Received: 14 September 2017 / Approved: 14 September 2017 / Online: 14 September 2017 (10:01:38 CEST)

A peer-reviewed article of this Preprint also exists.

Fu, Y.; Wang, J.-Y.; Zhang, D.; Chen, Y.-F.; Gao, S.; Zhao, L.-X.; Ye, F. Solvent-Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines. Molecules 2017, 22, 1601. Fu, Y.; Wang, J.-Y.; Zhang, D.; Chen, Y.-F.; Gao, S.; Zhao, L.-X.; Ye, F. Solvent-Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines. Molecules 2017, 22, 1601.

Abstract

A series of novel sulfonylurea benzothiazoline were designed by splicing active groups and bioisosterism. A solvent-free synthetic route was developed for the sulfonylurea benzothiazoline derivatives via the cyclization and carbamylation. All the compounds were characterized by IR, 1H-NMR, 13C-NMR, HRMS. The biological activity tests indicated the compounds could protect maize against the injury caused by chlorsulfuron to some extent. The molecular docking result showed that the new compound competed with chlorosulfuron to bind with the herbicide target enzyme active site to attain detoxification.

Keywords

active subunit combination; sulfonylurea benzothiazoline; solvent-free synthesis; safener activity

Subject

Chemistry and Materials Science, Organic Chemistry

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