The authors synthesized a series of novel 5-heterocycloxy-3-substituted-1-（3-trifluoromethyl）phenyl-1H- pyrazole derivatives. Herbicidal activities of the two intermediate compounds and thirteen target compounds wer...The authors synthesized a series of novel 5-heterocycloxy-3-substituted-1-（3-trifluoromethyl）phenyl-1H- pyrazole derivatives. Herbicidal activities of the two intermediate compounds and thirteen target compounds were evaluated via Brassica napus and Echinochloa crusgalli（L.） Beauv tests. Bioassay results show that some of the compounds exhibit better inhibiting activities against Brassica napus and some of the compounds exhibit bleaching activities against Echinochloa crusgalli（L.） Beauv at 100 μg/mL.展开更多
Xanthene and Xanthenediones are structural components of several bioactive and semi-synthetic molecules. This work described an expeditious synthesis of novel and hitherto unreported bis-trifluoromethyl xanthene dione...Xanthene and Xanthenediones are structural components of several bioactive and semi-synthetic molecules. This work described an expeditious synthesis of novel and hitherto unreported bis-trifluoromethyl xanthene dione derivatives. The reaction of two equivalents of 5-trifluoromethyl cyclohexane-1,3- dione with substituted aromatic aldehydes in the presence of ethanol containing 1 - 2 drops of HCl was facile under microwave irradiation. Short reaction time (25 min), good to excellent yields (80% - 95%), good atom economy, and simple workup are the major advantages of the above procedure. Moreover, the fluorinated products represent synthetically useful stable intermediates that could find applications in pharmaceutical, agricultural and material industries.展开更多
以L-丙氨酸和四氟化硫为原料,压力下经一步氟化反应制得α-三氟甲基乙胺。实验研究获得的最佳工艺条件为：以100 g L-丙氨酸为原料,n（L-丙氨酸）∶n（四氟化硫）为1∶2,55℃及18-19 kgf/cm^2压力下保温反应12 h,产品收率在55%以上,产...以L-丙氨酸和四氟化硫为原料,压力下经一步氟化反应制得α-三氟甲基乙胺。实验研究获得的最佳工艺条件为：以100 g L-丙氨酸为原料,n（L-丙氨酸）∶n（四氟化硫）为1∶2,55℃及18-19 kgf/cm^2压力下保温反应12 h,产品收率在55%以上,产品盐酸盐熔点在218.5℃以上。展开更多
The fused triazole derivatives,which is an important inhibitors of the dipeptidyl peptidase-Ⅳ enzyme(DPP-Ⅳ),can be used for the treatment or prevention of type 2 diabetes.A new fused triazole derivatives of 3-oxo-3-...The fused triazole derivatives,which is an important inhibitors of the dipeptidyl peptidase-Ⅳ enzyme(DPP-Ⅳ),can be used for the treatment or prevention of type 2 diabetes.A new fused triazole derivatives of 3-oxo-3-[3-trifluoromethyl-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-phenylpropan-1-amine was synthesized from 2-chloropyrazine and benzaldehyde by hydrazinolysis,trifluoroacetylation,cyclization,hydrogenation,condensation and deprotection reaction.The structures of the compound and its intermediates were determined by IR,NMR,and MS.展开更多
An efficient method for Cu-catalyzed decarboxylative trifluoromethylation offl-ketoacids to achieve a-trifluoro- methyl ketones was developed. A wide variety of synthetically useful α-trifluoromethyl ketones were obt...An efficient method for Cu-catalyzed decarboxylative trifluoromethylation offl-ketoacids to achieve a-trifluoro- methyl ketones was developed. A wide variety of synthetically useful α-trifluoromethyl ketones were obtained in modest to good yields under mild reaction conditions. The present method also exhibits good functional-group compatibility.展开更多
基金Support by the National Natural Science Foundation of China(Nos.21002054, 20572054)the Research Fund for the Doctoral Programme of Higher Education of China(No.20100031120016)the Fundamental Research Funds for the Central Universities of China
文摘The authors synthesized a series of novel 5-heterocycloxy-3-substituted-1-（3-trifluoromethyl）phenyl-1H- pyrazole derivatives. Herbicidal activities of the two intermediate compounds and thirteen target compounds were evaluated via Brassica napus and Echinochloa crusgalli（L.） Beauv tests. Bioassay results show that some of the compounds exhibit better inhibiting activities against Brassica napus and some of the compounds exhibit bleaching activities against Echinochloa crusgalli（L.） Beauv at 100 μg/mL.
文摘Xanthene and Xanthenediones are structural components of several bioactive and semi-synthetic molecules. This work described an expeditious synthesis of novel and hitherto unreported bis-trifluoromethyl xanthene dione derivatives. The reaction of two equivalents of 5-trifluoromethyl cyclohexane-1,3- dione with substituted aromatic aldehydes in the presence of ethanol containing 1 - 2 drops of HCl was facile under microwave irradiation. Short reaction time (25 min), good to excellent yields (80% - 95%), good atom economy, and simple workup are the major advantages of the above procedure. Moreover, the fluorinated products represent synthetically useful stable intermediates that could find applications in pharmaceutical, agricultural and material industries.
文摘The fused triazole derivatives,which is an important inhibitors of the dipeptidyl peptidase-Ⅳ enzyme(DPP-Ⅳ),can be used for the treatment or prevention of type 2 diabetes.A new fused triazole derivatives of 3-oxo-3-[3-trifluoromethyl-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-phenylpropan-1-amine was synthesized from 2-chloropyrazine and benzaldehyde by hydrazinolysis,trifluoroacetylation,cyclization,hydrogenation,condensation and deprotection reaction.The structures of the compound and its intermediates were determined by IR,NMR,and MS.
基金We gratefully acknowledge financial support from the National Natural Science Foundation of China （21472033） and the Fundamental Research Funds for the Central Universities. We thank Wen-Man Zhang and Bei Huang in this group for reproducing the results of compounds 3c, 3e, and 3m.
文摘An efficient method for Cu-catalyzed decarboxylative trifluoromethylation offl-ketoacids to achieve a-trifluoro- methyl ketones was developed. A wide variety of synthetically useful α-trifluoromethyl ketones were obtained in modest to good yields under mild reaction conditions. The present method also exhibits good functional-group compatibility.
