BACKGROUND: Glyphosate is the most widely used and successful herbicide discovered to date, but its utility is now threatened by the occurrence of several glyphosate-resistant weed species. Saflufenacil is a relatively new herbicide developed by BASF in 2010 and is a highly effective selective herbicide showing excellent control on broadleaf weeds (more than 90 species), significantly superior to other PPO inhibitor herbicides at the level of weeds controlled. It is also effective against glyphosate-resistant Conyza Canadensis if used in a combination with glyphosate. A series of novel uracil-based PPO inhibitors containing an isoxazoline moiety were designed via the Intermediate Derivatization Method (IDM), synthesized using a key saflufenacil raw material as starting material, and evaluated for herbicidal activity. RESULTS: The target compounds were characterized by 1 H NMR and HRMS. Bioassays indicated that some title compounds can control efficiently and effectively both broadleaf weeds and grassy weeds at low doses, especially glyphosate resistant weeds: Conyza canadensis and Eleusine indica. CONCLUSION: This work provides a basis for further studies of 9b for control of a wider range of weeds, particularly for glyphosate resistant weeds. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.
BACKGROUND:Glyphosate is the most widely used and successful herbicide discovered to date, but its utility is now threatened by the occurrence of several glyphosate-resistant weed species. Saflufenacil is a relatively new herbicide developed by BASF in 2010 and is a highly effective selective herbicide showing excellent control on broadleaf weeds (more than 90 species), significantly superior to other PPO inhibitor herbicides at the level of weeds controlled. It is also effective against glyphosate-resistant Conyza Canadensis if used in a combination with glyphosate. A series of novel uracil-based PPO inhibitors containing an isoxazoline moiety were designed via the Intermediate Derivatization Method (IDM), synthesized using a key saflufenacil raw material as starting material, and evaluated for herbicidal activity. RESULTS: The target compounds were characterized by 1 H NMR and HRMS. Bioassays indicated that some title compounds can control efficiently and effectively both broadleaf weeds and grassy weeds at low doses, especially glyphosate resistant weeds: Conyza canadensis and Eleusine indica. CONCLUSION: This work provides a basis for further studies of 9b for control of a wider range of weeds, particularly for glyphosate resistant weeds. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.