Guan-fu base A(GFA),a new antiarrhythmic alkaloid with a structure of C_(20)-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride(TFAA) to produce GFA—TFAA of which the structure was iden...Guan-fu base A(GFA),a new antiarrhythmic alkaloid with a structure of C_(20)-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride(TFAA) to produce GFA—TFAA of which the structure was identified by GC—MSD.There was a wide linear range of the GC-ECD method from 10 to 20000ng/ml(r=0.9984).The average recovery of GFA from the spiked plasma was 97.52%.The coefficients of variation of within-day and between-day were less than 7% and 9%,respectively.The method was used in the preclinical experiment of pharmacology of GFA and the results showed that GFA con- centrations in rabbits' plasma within 6 hours after the administration ranged from 0.338± 0.014 to 13.459±5.393μg/ml for dosage 10mg/kg,from 0.133±0.038 to 2.546±0.480 μg/ml for dosage 2mg/kg and from 45.25±10.34 to 535.86±24.36ng/ml for dosage 0.4 mg/kg.展开更多
We report the first trifluoroacetic anhydride- and trifluoroacetic acid-promoted cascade reaction with phtoroglucinoltribenzyl ether and carboxylic acid as starting materials. By simply varying the temperature of syst...We report the first trifluoroacetic anhydride- and trifluoroacetic acid-promoted cascade reaction with phtoroglucinoltribenzyl ether and carboxylic acid as starting materials. By simply varying the temperature of systems containing the same starting materials, different products were produced in high yields. A three-step consecutive reaction process was also proposed.展开更多
Fluoroalkyl-containing organic compounds have exhibited wide applications in the field of pharmaceuticals,agrochemicals and materials science due to their outstanding properties such as biological activity,metabolic s...Fluoroalkyl-containing organic compounds have exhibited wide applications in the field of pharmaceuticals,agrochemicals and materials science due to their outstanding properties such as biological activity,metabolic stability,lipophilicity,excellent chemical and thermal stability.Therefore,various synthetic strategies have been developed for the construction of fluoroalkyl-containing compounds,using highly active fluorinating reagents and fluorinated building blocks.Recently,the use of easily available and inexpensive trifluoroacetic anhydride(TFAA)and its anhydride analogues has attracted great attention to access numerous fluoroalkyl-containing compounds through cyclization and coupling reactions.In this review,we summarized the recent advances in the synthesis of fluoroalkylated compounds using fluoroalkyl anhydrides as reagents.This review aims to provide a reference for researchers on how to develop new synthetic straregies of fluorine-containing organic compounds and achieve kilograms or even tons preparation of fluorine-containing organic compounds using fluoroalkyl anhydrides.展开更多
文摘Guan-fu base A(GFA),a new antiarrhythmic alkaloid with a structure of C_(20)-diterpenoid could react rapidly and quantitatively with trifluoroacetic anhydride(TFAA) to produce GFA—TFAA of which the structure was identified by GC—MSD.There was a wide linear range of the GC-ECD method from 10 to 20000ng/ml(r=0.9984).The average recovery of GFA from the spiked plasma was 97.52%.The coefficients of variation of within-day and between-day were less than 7% and 9%,respectively.The method was used in the preclinical experiment of pharmacology of GFA and the results showed that GFA con- centrations in rabbits' plasma within 6 hours after the administration ranged from 0.338± 0.014 to 13.459±5.393μg/ml for dosage 10mg/kg,from 0.133±0.038 to 2.546±0.480 μg/ml for dosage 2mg/kg and from 45.25±10.34 to 535.86±24.36ng/ml for dosage 0.4 mg/kg.
基金Supported by the National Natural Science Foundation of China（No.51209024）.
文摘We report the first trifluoroacetic anhydride- and trifluoroacetic acid-promoted cascade reaction with phtoroglucinoltribenzyl ether and carboxylic acid as starting materials. By simply varying the temperature of systems containing the same starting materials, different products were produced in high yields. A three-step consecutive reaction process was also proposed.
基金supported by the National Natural Science Foundation of China(Nos.21772022,and 22171124)Minjiang University(No.MJY21041)Fuzhou University.
文摘Fluoroalkyl-containing organic compounds have exhibited wide applications in the field of pharmaceuticals,agrochemicals and materials science due to their outstanding properties such as biological activity,metabolic stability,lipophilicity,excellent chemical and thermal stability.Therefore,various synthetic strategies have been developed for the construction of fluoroalkyl-containing compounds,using highly active fluorinating reagents and fluorinated building blocks.Recently,the use of easily available and inexpensive trifluoroacetic anhydride(TFAA)and its anhydride analogues has attracted great attention to access numerous fluoroalkyl-containing compounds through cyclization and coupling reactions.In this review,we summarized the recent advances in the synthesis of fluoroalkylated compounds using fluoroalkyl anhydrides as reagents.This review aims to provide a reference for researchers on how to develop new synthetic straregies of fluorine-containing organic compounds and achieve kilograms or even tons preparation of fluorine-containing organic compounds using fluoroalkyl anhydrides.
