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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

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Qilian Mountain permafrost, with area about 10×104 km2, locates in the north of Qinghai‐Tibet plateau. It equips with perfect conditions and has great prospecting potential for gas hydrate. The Scientific Drilling Project of Gas Hydrate in Qilian Mountain permafrost, which locates in Juhugeng of Muri Coalfield, Tianjun County, Qinghai Province, has been implemented by China Geological Survey in 2008–2009. Four scientific drilling wells have been completed with a total footage of 2059.13 m. Samples of gas hydrate are collected separately from holes DK‐1, DK‐2 and DK‐3. Gas hydrate is hosted under permafrost zone in the 133–396 m interval. The sample is white crystal and easily burning. Anomaly low temperature has been identified by the infrared camera. The gas hydrate‐bearing cores strongly bubble in the water. Gas‐bubble and water‐drop are emitted from the hydrate‐bearing cores and then characteristic of honeycombed structure is left The typical spectrum curve of gas hydrate is detected using Raman spectrometry. Furthermore, the logging profile also indicates high electrical resistivity and sonic velocity. Gas hydrate in Qilian Mountain is characterized by a thinner permafrost zone, shallower buried depth, more complex gas component and coal‐bed methane origin etc.

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Strobilurin derivatives have become one of the most important classes of agricultural fungicide due to a novel action mode, wide fungicidal spectrum, lower toxicity toward mammalian cells, and environmentally benign characteristics. To discover new strobilurin analogues with high activity against resistant pathogens, a series of new chalcone-based strobilurin derivatives are designed and synthesized by integrating a chalcone scaffold with a strobilurin pharmacophore. The preliminary bioassay showed that some of the chalcone analogues exhibited good in vivo fungicidal activities against Pseudoperoniospora cubensis and Sphaerotheca fuliginea at the dosage of 200 microg mL(-1). Two compounds, (E)-methyl 2-[2-({3-[(E)-3-(2-chlorophenyl)acryloyl]phenoxy}methyl)phenyl]-3-methoxyacrylate (1e) and (E)-methyl 2-[2-({3-[(E)-3-(3-bromophenyl)acryloyl]phenoxy}methyl)phenyl]-3-methoxyacrylate (1l), were found to display higher fungicidal activities against P. cubensis (EC90=118.52 microg mL(-1) for 1e and EC90=113.64 microg mL(-1) for 1l) than Kresoxim-methyl (EC90=154.92 microg mL(-1)) and were identified as the most promising candidates for further study. The present work demonstrated that strobilurin analogues containing chalcone as a side chain could be used as a lead structure for further developing novel fungicides. To our knowledge, this is the first report about the syntheses and fungicidal activities of chalcone-based strobilurin derivatives.

The pyrimidinamine diflumetorim is an ideal template for the discovery of agrochemical lead compounds due to its unique mode of action, novel chemical structure, and lack of reported resistance. To develop a new pyrimidinamine fungicide effective against cucumber downy mildew (CDM), a series of new pyrimidinamine derivatives containing an aryloxy pyridine moiety were designed and synthesized by employing the recently reported intermediate derivatization method (IDM). The structures of all compounds were identified by H NMR, elemental analyses, HRMS, and X-ray diffraction. Bioassays demonstrated that some of the title compounds exhibited excellent fungicidal activities against CDM. Compound 9 gave the best activity (EC = 0.19 mg/L), which is significantly better than the commercial fungicides diflumetorim, flumorph, and cyazofamid. The relationship between structure and fungicidal activity of the synthesized pyrimidinamines was explored. The study showed that compound 9 is a promising fungicide candidate for further development.