2989-17-5Relevant articles and documents
Preparation method of 2-methyl-4-chloro-phenoxyacetic acid
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Paragraph 0028-0031; 0034-0035; 0046-0055, (2020/09/21)
The invention belongs to the technical field of pesticide synthesis, and particularly relates to a 2-methyl-4-chloro-phenoxyacetic acid preparation method, which uses o-methylphenol sodium as a reactant, and uses an organic phase methyl chloroacetate solution as a reaction solvent in a condensation reaction. The method has the advantages that the method is simple; in the condensation reaction, anorganic phase methyl chloroacetate solution is used as a reaction solvent to replace a water phase in the traditional technology; and the organic phase can be continued to the subsequent chlorinationreaction, so that the problems of decomposition of sodium chloroacetate and low reaction yield can be solved, no wastewater can be generated in the production of MCPA sodium salt, the yield can be greatly improved, and the method is a green and environment-friendly synthesis method.
Preparation method of phenoxyacetic ester
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Paragraph 0056; 0057; 0058; 0059; 0087-0090, (2019/01/08)
The invention provides a preparation method of phenoxyacetic ester, wherein the preparation method includes the following steps: A) carrying out esterification reaction of acetic acid and alcohol to obtain acetic ester; B) introducing chlorine gas into acetic ester, and carrying out reaction to obtain chloroacetic ester; C) dehydrating a phenol compound and alkaline hydroxide into a salt in an organic solvent to obtain a salt of the phenol compound; D) after salt formation, mixing with chloracetic ester prepared in the step B), and carrying out condensation reaction to obtain phenoxyacetic ester, wherein the organic solvent is a mixture of any two kinds of toluene, xylene, chlorobenzene, phenol, butanol and isobutanol. The phenol is dehydrated into the salt in the mixed organic solvent, the system still maintains a uniform state in the dehydration process, continuous production is achieved, the dehydration efficiency is high and the efficiency of the whole production process is high. Moreover, the raw materials are easy to obtain, the production period is short, water is not needed in the reaction process, the energy consumption is low, the production cost is low, the yield of acetic acid is 99% or more, and the total yield of phenol can reach 99% or more.
Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists
Wang, Xuekun,Zhao, Tianxiao,Yang, Baowei,Li, Zheng,Cui, Jian,Dai, Yuxuan,Qiu, Qianqian,Qiang, Hao,Huang, Wenlong,Qian, Hai
, p. 132 - 140 (2015/02/18)
Free fatty acid receptor 1 (FFA1) is a new potential drug target for the treatment of type 2 diabetes because of its role in amplifying glucose-stimulated insulin secretion in pancreatic β-cell. In the present studies, we identified phenoxyacetic acid derivative (18b) as a potent FFA1 agonist (EC50 = 62.3 nM) based on the structure of phenylpropanoic acid derivative 4p. Moreover, compound 18b could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice without observation of hypoglycemic side effect. Additionally, compound 18b exhibited acceptable PK profiles. In summary, compound 18b with ideal PK profiles exhibited good activity in vitro and in vivo, and might be a promising drug candidate for the treatment of diabetes mellitus.
