Design, synthesis and structure–activity relationship of novel diphenylamine derivatives

Design, synthesis and herbicidal evaluation of novel uracil derivatives containing an isoxazoline moiety

“…7 The intermediate derivatization method (IDM) is a useful and highly efficient approach for agrochemical discovery. [8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24] Using this approach, novel molecules are constructed based on one or more chemical intermediates identified by retrosynthesis analysis. Applying such an analysis to saflufenacil, we found that saflufenacil can be produced starting from 2-chloro-4-fluorotoluene by oxidation, nitration, reduction and cyclization reactions, thus 2-chloro-4-fluorotoluene is a key raw material.…”

Synthesis and biological activity of pyridazine amides, hydrazones and hydrazides

“…Fortunately, a diverse set of tools is available to scientists. These tools include designing compounds based on target sites or modes‐of‐action, using natural products as starting points, modification of known bioactive scaffolds, and fragment‐based approaches …”

“…These tools include designing compounds based on target sites or modes-of-action, 7 using natural products as starting points, modification of known bioactive scaffolds, and fragment-based approaches. 8 Another approach toward the discovery of novel insecticidal compounds is to employ high-throughput screening of diverse or structurally focused sets of chemistry for activity against insect pests. 9 The availability of commercial compound collections makes this approach an attractive one.…”

“….25 N ′ -Methyl-N ′ - [6-(3-pyridyl)pyridazin-3-yl]benzohydrazide (55) Isolated as a white solid in 35% yield. mp 188-190 ∘ C. 1 H NMR (400 MHz, CDCl 3 ) 9.11 (m, 1H, pyridine), 8.83 (s, 1H, NH), 8.64 (m, 1H, pyridine), 8.34 (dt, J = 8.0, 1.9 Hz, 1H, pyridine), 7.91 (m, 2H, phenyl), 7.67 (d, J = 9.5 Hz, 1H, pyridazine), 7.60 (m, 1H, phenyl), 7.50 (t, J = 7.6 Hz, 2H, phenyl), 7.40 (dd, J = 8.0, 4.8 Hz, 1H, pyridine), 7.11 (d, J = 9.5 Hz, 1H, pyridazine), 3.63 (s, 3H, NCH 3 ). ; ESIMS m/z 306.0 ([M+H] + ).…”

Intermediate derivatisation method in the discovery of new acaricide candidates: synthesis of N‐substituted piperazine derivatives and their activity against phytophagous mites

“…), were obtained by intermediate derivatisation methods (IDMs) – a practical approach to agrochemical discovery . IDMs use a three‐pronged approach to agrochemical discovery – the common intermediate method (CIM), the terminal group replacement method (TRM or RM) and the active compound derivatisation method (ADM or DM) . Among these three approaches, the common intermediate method has proved to be an effective and practical method .…”