Tert-Amino effect: The Meth-Cohn and Reinhoudt reactions (Review)

The data published over the last 15-20 years on reactions taking place by the tert-amino effect mechanism have been reviewed. © 2013 Springer Science+Business Media New York

Synthesis of 1,2,3-Thiadiazole and Thiazole-Based Strobilurins as Potent Fungicide Candidates

Strobilurin fungicides play a crucial role in protecting plants against different pathogens and securing food supplies. A series of 1,2,3-thiadiazole and thiazole-based strobilurins were rationally designed, synthesized, characterized, and tested against various fungi. Introduction of 1,2,3-thiadiazole greatly improved the fungicidal activity of the target molecules. Compounds <b>8a</b>, <b>8c</b>, <b>8d</b>, and <b>10i</b> exhibited a relatively broad spectrum of fungicidal activity. Compound <b>8a</b> showed excellent activities against Gibberella zeae, Sclerotinia sclerotiorum, and Rhizoctonia cerealis with median effective concentrations (EC₅₀) of 2.68, 0.44, and 0.01 μg/mL, respectively; it was much more active than positive controls enestroburin, kresoxim-methyl, and azoxystrobin with EC₅₀ between 0.06 and 15.12 μg/mL. Comparable or better fungicidal efficacy of compound <b>8a</b> compared with azoxystrobin and trifloxystrobin against Sphaerotheca fuliginea and Pseudoperonspera cubensis was validated in cucumber fields at the same application dosages. Therefore, compound <b>8a</b> is a promising fungicidal candidate worthy of further development

Synthesis of 1,2,3-Thiadiazole and Thiazole-Based Strobilurins as Potent Fungicide Candidates

Strobilurin fungicides play a crucial role in protecting plants against different pathogens and securing food supplies. A series of 1,2,3-thiadiazole and thiazole-based strobilurins were rationally designed, synthesized, characterized, and tested against various fungi. Introduction of 1,2,3-thiadiazole greatly improved the fungicidal activity of the target molecules. Compounds <b>8a</b>, <b>8c</b>, <b>8d</b>, and <b>10i</b> exhibited a relatively broad spectrum of fungicidal activity. Compound <b>8a</b> showed excellent activities against Gibberella zeae, Sclerotinia sclerotiorum, and Rhizoctonia cerealis with median effective concentrations (EC₅₀) of 2.68, 0.44, and 0.01 μg/mL, respectively; it was much more active than positive controls enestroburin, kresoxim-methyl, and azoxystrobin with EC₅₀ between 0.06 and 15.12 μg/mL. Comparable or better fungicidal efficacy of compound <b>8a</b> compared with azoxystrobin and trifloxystrobin against Sphaerotheca fuliginea and Pseudoperonspera cubensis was validated in cucumber fields at the same application dosages. Therefore, compound <b>8a</b> is a promising fungicidal candidate worthy of further development