167408-63-1

Upstream product

• 42957-17-5 methyl 5,5-dimethyl-2,4-dioxohexanoate 
• 77-78-1 dimethyl sulfate 
• 75-97-8 3,3-dimethyl-butan-2-one 
• 67-56-1 methanol 
• 175277-11-9 3-(tert-butyl)-1-methyl-1H-pyrazole-5-carboxylic acid 

Relevant academic research and scientific papers

Ligand-Promoted C(sp3)-H Olefination en Route to Multi-functionalized Pyrazoles

A Pd-catalyzed/N-heterocycle-directed C(sp3)-H olefination has been developed. The monoprotected amino acid ligand (MPAA) is found to significantly promote Pd-catalyzed C(sp3)-H olefination for the first time. Cu(OAc)2 instead of Ag+ salts are used as the terminal oxidant. This reaction provides a useful method for the synthesis of alkylated pyrazoles. The right moves: A pyrazole-directed C(sp3)-H olefination has been developed (see scheme). The monoprotected amino acid ligands (MPAA) are found to significantly promote the reactivity in Pd-catalyzed C(sp3)-H olefination. The applicability of using this reaction for late-stage diversification of pyrazole-based complex scaffold is demonstrated.

Synthesis, Acaricidal Activity, and Structure-Activity Relationships of Pyrazolyl Acrylonitrile Derivatives

A series of novel pyrazolyl acrylonitrile derivatives was designed, targeting Tetranychus cinnabarinus, and synthesized. Their structures were identified by combination of1H NMR,13C NMR, and MS spectra. The structures of compounds 18 and 19 were further confirmed by X-ray diffraction. Extensive greenhouse bioassays indicated that compound 19 exhibits excellent acaricidal activity against all developmental stages of T. cinnabarinus, which is better than the commercialized compounds cyenopyrafen and spirodiclofen. It was shown that the acute toxicity of compounds 19 to mammals is quite low. The structure-activity relationships are also discussed.