57061-71-9Relevant articles and documents
Preparation method of flibaserin hydrochloride
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, (2020/07/15)
The invention relates to the technical field of synthesis of medical intermediates, particularly to a preparation method of flibaserin hydrochloride. According to the preparation method, o-phenylenediamine and 3-trifluoromethylphenylpyrazine are used as raw materials; o-phenylenediamine reacts with ethyl acetoacetate to obtain a compound 10-1-G; the 3-trifluoromethylphenylpyrazine compound I is subjected to a two-step substitution reaction to obtain a compound 10-1-B; and the compound 10-1-B and the compound 10-1-G are subjected to a substitution reaction to obtain a final product compound flibaserin hydrochloride. The invention aims to reduce the cost, optimize the process and facilitate industrial production. The method is simple and convenient to operate, reasonable in reaction process,low in production cost, good in product quality, free of environmental pollution and suitable for industrial production, wherein the content of the product is higher than 99.5%.
A new method for synthesizing flibanserin (by machine translation)
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Paragraph 0052; 0060; 0061; 0070; 0076; 0077; 0081; 0087, (2019/02/04)
The invention relates to a new method for synthesizing of flibanserin, which belongs to the technical field of organic synthesis. The invention respectively in order to triethanolamine and between amino benzotrifluoride as the starting material, to prepare the piperazine intermediate; then to the O-phenylene diamine and the original four carbonate as raw material, the preparation of the ethoxy and imidazole intermediate; the obtained piperazine intermediate and benzimidazole intermediate undergo the substitution reaction, and hydrochloric acid deprotection to obtain the target product of flibanserin. The invention has few synthetic steps, few by-products, intermediate products and the target product yield is relatively high, intermediate product 2 - ethoxy and imidazole yield up 94.2%, the target product yield can reach 56.2%, it can be seen, the invention overcomes the substance in the prior art synthesis step is tedious, and more byproducts, target low yield of product defect. In addition, the present invention has a simple structure, high purity of product, the economic and environmental protection industrial line, has a very wide range of use and potential economic benefits. (by machine translation)
Preparation method of flibaserin intermediate
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Paragraph 0036; 0037; 0038; 0039; 0040; 0041; 0042-0044, (2017/07/19)
The invention discloses a method belonging to the field of heterocyclic compounds, and concretely relates to a preparation method of a flibaserin intermediate. The preparation method comprises the following steps of (1) dissolving 1-(3-trifluoromethylphenyl) piperazine hydrochloride in a solvent a, and reacting with 2-halogenated ethanol or ethylene oxide in the presence of alkali to obtain 2-(4-(3-trifluoromethylphenyl) piperazine-1-ethanol; (2) reacting the 2-(4-(3-trifluoromethylphenyl) piperazine-1-ethanol with a chloride agent compound to obtain a compound as shown in a formula I. According to the preparation method, the reaction selectivity is improved, the generation of impurities is reduced, the product purity is improved, and the preparation method is simple and convenient to operate, environmentally-friendly, and beneficial for industrialized mass production.