Studies On The Synthesis And Biological Activities Of Phenoxy Carboxylic Acid And Isothiazolone Derivatives

The phenoxy carboxylic acid and the isothiazolone derivatives have important biological activities. The phenoxy carboxylic acid derivatives have extensive application and the research values in the agriculture, forestry and environment. The isothiazolone derivatives have extensive application and the research values in the medicine, agriculture, cosmetics, textile product etc. It is a very important target to obtain more compounds which have higher effect, wider application, better selectivity and lower toxicity. This article concentrates on the synthesis of the phenoxy carboxylic acid derivatives and the synthesis and biological activities of the isothiazolone derivatives. 14 phenoxy carboxylic acid derivatives including 11 new compounds have been synthesized; 10 isothiazolone derivatives including 7 new compounds have been synthesized. All of the target compounds have been isolated and characterized by IR, 1HNMR, MS and elemental analysis. The following innovated results were achieved: (1) 5 phenoxy acetic acid derivatives have been designed and synthesized. 3 of them were reported for the first time and their structures have been confirmed by 1H NMR, elemental analysis, MS and IR. (2) 8 phenoxy propionic acid derivatives have been designed and synthesized. 7 of them were reported for the first time and their structures have been confirmed by 1H NMR, MS, IR and elemental analysis. (3) One new heterocyclic phenoxy propionic acid derivatives were synthesized isolated and characterized by IR, 1HNMR, MS and elemental analysis. The study gives a good basis to expand the research and applications of the phenoxy carboxylic acid ester derivatives. (4) One non-haloid isothiazolone compound, 2 chlorin-substituted isothiazolone derivatives and one dichlorin-substituted isothiazolone derivative have been synthesized. 3 of them were reported for the first time and their structures have been confirmed by 1H NMR, MS, IR and elemental analysis. (5) 3 bromine-substituted isothiazolone derivatives and 3 bromine-and chlorine-substituted isothiazolone derivatives have been synthesized. 4 of them were reported for the first time and their structures have been confirmed by 1H NMR, MS, IR and elemental analysis. (6) Anti-bacteria activity of eight isothiazolone compounds against five bacteria was tested and the following results were obtained: a) all of the tested compounds have strong anti-bacteria activity. b) It is always advantageous to the anti-bacteria activity to increase the number of halogen atom in the molecule. c) The bigger group on 2-position is advantageous to enhance the anti-bacteria activity of molecule.