In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitutio...In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitution, reduction and acylation procedures. Preliminary bioassay showed that all the target compounds processing good anti-TMV （tobacco mosaic virus） activity. Two compounds （4d and 4e） displayed higher activity superior to virazole at a concentration of 5.0 ×10^-4 g/mE.展开更多
Plant growth regulators(PGRs)are chemical substances that imitate the functions of phytohormones to enhance the crop yield and the harvest process.Phenylurea-derived plant growth regulators are known for their excelle...Plant growth regulators(PGRs)are chemical substances that imitate the functions of phytohormones to enhance the crop yield and the harvest process.Phenylurea-derived plant growth regulators are known for their excellent efficacy in promoting fruit growth,particularly in kiwifruit,grapes,and melons.Phenylurea derivatives represent one class of the highly efficient and versatile PGRs.Specifically,forchlorfenuron(CPPU,N-(2-chloro-4-pyridinyl)-N0-phenylurea)exhibits similar growth-regulating efficacy to cytokinins and has a significant impact on the plant growth and the crop yield.As a result,there is growing interest in exploring the incorporation of various phenylurea moieties into agrochemicals to enhance their regulatory properties on crops.This review aims to provide a comprehensive overview on representative synthetic approaches for phenylurea derived PGRs.Additionally,we provide our perspective on the future development in this active researchfield.展开更多
A novel environmentally benign process for the synthesis of methyl N-phenyl carbamate (MPC) from methanol and phenylurea was studied. Effect of solvent and catalyst on the reaction behavior was investigated. The IR s...A novel environmentally benign process for the synthesis of methyl N-phenyl carbamate (MPC) from methanol and phenylurea was studied. Effect of solvent and catalyst on the reaction behavior was investigated. The IR spectra of methanol and phenylurea dissolved in different solvents were also recorded. Compared with use of methanol as both a reactant and a solvent, phenylurea conversion and selectivity to MPC increased by using toluene, benzene or anisole as a solvent, while phenylurea conversion decreased slightly by using n-octane as a solvent. The phenylurea conversion declined nearly 50% when dimethyl sulfoxide (DMSO) was used as a reaction media, and MPC selec- tivity decreased as well. The catalytic reaction tests showed that a basic catalyst enhanced the selectivity to MPC while an acidic catalyst promoted the formation of methyl carbamate and aniline. Moderate degree of basicity showed the best catalytic performance in the cases studied.展开更多
wenty-eight new N-2-thiazolyl and thiazolinyl-N'-substituted phenylureaswere synthesized by the reaction of the heterocycles and substituted phenyl iso-cyanates. Their cytokinin activity was examined by cucumber c...wenty-eight new N-2-thiazolyl and thiazolinyl-N'-substituted phenylureaswere synthesized by the reaction of the heterocycles and substituted phenyl iso-cyanates. Their cytokinin activity was examined by cucumber cotyledon expansionbioassay. N-thiazolyl and N-thiazolinyl-N'-(m-chlorophenyl )-ureas showed a goodPGR activity in comparison to Kinetin. The structure/activity relationship was dis-cussed.展开更多
基金the the National 11th-Five-year Science and Technology Support Project on Pesticide Innovation (No.2006BAE01A01-1104)National Natural Science Foundation of China(No.20672138+1 种基金No.20902107)the Research Innovation Foundation of China Agricultural University(No.2006009)
文摘In order to find novel leading structures of pesticide, a series of N-（pyrimidin-5-yl）-N1-phenylureas （4a-4h） were designed and synthesized from 4-chloro-2-diethylamino-6-methyl-5-nitropyrimidine 1 via substitution, reduction and acylation procedures. Preliminary bioassay showed that all the target compounds processing good anti-TMV （tobacco mosaic virus） activity. Two compounds （4d and 4e） displayed higher activity superior to virazole at a concentration of 5.0 ×10^-4 g/mE.
基金support from the National Natural Science Foundation of China(22371058,21961006,32172459,22371057,22071036)the National Key Research and Development Program of China(2022YFD1700300)+3 种基金the Science and Technology Department of Guizhou Province(Qiankehejichu-ZK[2021]Key033)the Program of Introducing Talents of Discipline to Universities of China(111 Program,D20023)at Guizhou University,Frontiers Science Center for Asymmetric Synthesis and Medicinal MoleculesDepartment of Education,Guizhou Province[Qianjiaohe KY(2020)004]Guizhou University(China).
文摘Plant growth regulators(PGRs)are chemical substances that imitate the functions of phytohormones to enhance the crop yield and the harvest process.Phenylurea-derived plant growth regulators are known for their excellent efficacy in promoting fruit growth,particularly in kiwifruit,grapes,and melons.Phenylurea derivatives represent one class of the highly efficient and versatile PGRs.Specifically,forchlorfenuron(CPPU,N-(2-chloro-4-pyridinyl)-N0-phenylurea)exhibits similar growth-regulating efficacy to cytokinins and has a significant impact on the plant growth and the crop yield.As a result,there is growing interest in exploring the incorporation of various phenylurea moieties into agrochemicals to enhance their regulatory properties on crops.This review aims to provide a comprehensive overview on representative synthetic approaches for phenylurea derived PGRs.Additionally,we provide our perspective on the future development in this active researchfield.
基金Project supported by the Science and Technology Ministry of China (No. 2001CCA02700).
文摘A novel environmentally benign process for the synthesis of methyl N-phenyl carbamate (MPC) from methanol and phenylurea was studied. Effect of solvent and catalyst on the reaction behavior was investigated. The IR spectra of methanol and phenylurea dissolved in different solvents were also recorded. Compared with use of methanol as both a reactant and a solvent, phenylurea conversion and selectivity to MPC increased by using toluene, benzene or anisole as a solvent, while phenylurea conversion decreased slightly by using n-octane as a solvent. The phenylurea conversion declined nearly 50% when dimethyl sulfoxide (DMSO) was used as a reaction media, and MPC selec- tivity decreased as well. The catalytic reaction tests showed that a basic catalyst enhanced the selectivity to MPC while an acidic catalyst promoted the formation of methyl carbamate and aniline. Moderate degree of basicity showed the best catalytic performance in the cases studied.
文摘wenty-eight new N-2-thiazolyl and thiazolinyl-N'-substituted phenylureaswere synthesized by the reaction of the heterocycles and substituted phenyl iso-cyanates. Their cytokinin activity was examined by cucumber cotyledon expansionbioassay. N-thiazolyl and N-thiazolinyl-N'-(m-chlorophenyl )-ureas showed a goodPGR activity in comparison to Kinetin. The structure/activity relationship was dis-cussed.
