Preprint Article Version 1 NOT YET PEER-REVIEWED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)

How to cite: Fu, Y.; Wang, J.; Zhang, D.; Chen, Y.; Gao, S.; Zhao, L.; Ye, F. Solvent Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines. Preprints 2017, 2017090056 (doi: 10.20944/preprints201709.0056.v1). Fu, Y.; Wang, J.; Zhang, D.; Chen, Y.; Gao, S.; Zhao, L.; Ye, F. Solvent Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines. Preprints 2017, 2017090056 (doi: 10.20944/preprints201709.0056.v1).

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.

Subject Areas

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

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