Application of the Intermediate Derivatization Approach in Agrochemical Discovery

Abstract

CONTENTS 7097 3.2. Discovery of Advanced Candidates SYP-1545, SYP-4288, and SYP-4380 7098 4. Conclusion 7098 Author Information 7099 Corresponding Author 7099 Present Address 7099 Notes 7099 Biographies 7099 Acknowledgments 7100 References 7100

Design, Synthesis and Antifungal Activity of Coumarin Ring-Opening Derivatives

“…As the structural core, coumarin occurs widely in natural products, drugs and agrochemicals (Figure 1), these important applications have generated considerable interest in this ring system and various fused coumarin derivatives have been reported [3][4][5][6]: Osthole, a natural O-methylated coumarin found in Cnidium Monnieri, a traditional Chinese herbal medicine that has been used as as a fungicidein China for a long history,and shows antifungal activity against Rhizoctonia solani and a broad spectrum of other phytopathogenic fungi [7][8][9]; Warfarin and Acenocoumarol are anticoagulants normally used in the prevention of thrombosis and thromboembolism, function as the vitamin K antagonists [10][11][12]; and Coumoxystrobin (SYP-3375) is a coumarin-containing strobilurin fungicide that contains an (E)-methyl 3-methoxy-2-phenylacrylate substructure and displays a broad spectrum of antifungal activity [13][14][15]. In our previous work, Osthole was used as the lead structure to carry out structural optimization, and some synthesized furan [3,2-c]coumarin derivatives showed potent antifungal activity [16][17][18].…”

Design, synthesis and insecticidal evaluation of aryloxy dihalopropene derivatives

“…[4][5][6][7] Among these three approaches, the terminal group replacement method has been proven as an effective and practical method. [8][9][10][11][12][13][14][15][16][17][18][19] It is well-known that the aryloxyphenyl derivatives have been widely used in agriculture.…”

Design, Synthesis and Bioactivities of Novel Dichloro-Allyloxy-Phenol-Containing Pyrazole Oxime Derivatives

“…Therefore, researchers have to search for novel, efficient, and low toxicity insecticides. In view on the facts above, the authors sought to incorporate the dichloro-allyloxy-phenol moiety into pyrazole oxime molecules by the intermediate derivatisation method [23]. In the present work, a series of novel dichloro-allyloxy-phenol-containing pyrazole oxime compounds were synthesized, and their acaricidal and insecticidal activities were screened briefly.…”