167933-07-5Relevant articles and documents
Synthetic method of flibaserin
-
Paragraph 0038-0039; 0041; 0043-0044; 0046-0047; 0049-0050, (2021/09/21)
The invention relates to a synthesis method of flibaserin, and belongs to the technical field of organic synthesis. The method comprises the following steps: by taking methyl anthranilate as an initial raw material, firstly carrying out amido alkylation reaction on the methyl anthranilate and 1-(2-chloroethyl)-4-[3-(trifluoromethyl) phenyl] piperazine dihydrochloride under the action of alkali, then, carrying out alkaline hydrolysis to remove methyl ester, and finally, carrying out schmidt reaction under the action of diphenylphosphoryl azide to obtain the flibaserin. The method is novel in route design, short in synthesis step and few in by-products; and the method has the advantages of simple operation, simple post-treatment process, low requirements on reaction equipment, cheap and easily available raw materials, economy, environmental protection and suitableness for industrial production.
Preparation method of Flibanserin intermediate
-
, (2019/03/15)
The invention discloses a preparation method of a Flibanserin intermediate. The preparation method comprises: preparing 2-(4-(3-trifluoromethylphenyl)piperazine-1-ethanol from a hydrochloride of 1-(3-trifluoromethyl-phenyl)piperazine and 2-haloethanol or
A new method for synthesizing flibanserin (by machine translation)
-
Paragraph 0052; 0062; 0069; 0070; 0078; 0079; 0080; 0081, (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)
N-Arylation of DABCO with Diaryliodonium Salts: General Synthesis of N-Aryl-DABCO Salts as Precursors for 1,4-Disubstituted Piperazines
Bugaenko, Dmitry I.,Yurovskaya, Marina A.,Karchava, Alexander V.
, p. 6389 - 6393 (2018/10/09)
Employing DABCO as a substrate, aryl(mesityl)iodonium triflates are introduced as arylating agents for a tertiary sp3-nitrogen. Mild conditions and exceptional selectivity of the aryl group transfer allow unprecedented N-aryl-DABCO salts to be obtained, bearing substituents of different electronic natures. This metal-free methodology has no analogy among known transition-metal-based reactions. The utility of isolated N-aryl-DABCO salts is demonstrated for the preparation of flibanserin.
Preparation method of flibaserin
-
, (2018/09/14)
The invention relates to a preparation method of flibaserin. The method comprises the specific steps of taking o-phenylenediamine, ethyl acetoacetate, 1, 2-dibromoethane, piperazine and bromobenzotrifluoride as materials, and performing ring closing reaction, amination reaction, amination reaction, deprotection reaction and coupling reaction on the materials, so as to form flibaserin. The preparation method is high in yield, low in cost, easy to operate and suitable for industrialization.
A new process for preparing flibanserin (by machine translation)
-
, (2017/10/07)
The invention discloses a new process for preparing of flibanserin. The craft in order to 1 - benzyl or substituted benzyl - 2 - benzimidazolone as raw materials, first with 1, 2 - Dibromoethane reaction, to produce intermediate 1, intermediate 1 with 1 - (3 - trifluoromethylphenyl) piperazine salt to produce intermediate 2, intermediate 2 in presence of catalyst hydrogenation to remove the protecting group to obtain the flibanserin, the method cheap, simple operation method, mild reaction conditions, with potential industrial value. Wherein R1 , R2 , R3 , R4 , R5 The following substituent selected from the group H, CH3 , Cl, Br, OCH3 . (by machine translation)
A new process for preparing flibanserin (by machine translation)
-
, (2017/08/29)
The invention discloses a new process for preparing of flibanserin. In order to 1 - isopropenyl - 2 - benzimidazolone as raw materials, first with 2 - bromo ethanol reaction, to produce intermediate 1, intermediate 1 generated by the reaction with a sulfo
The preparation method of the flibanserin
-
, (2017/08/24)
The invention discloses a preparation method of flibanserin. The preparation method uses trifluoromethylbenzene, triamine (2-halogen ethyl) and ortho-nitroaniline which are easy to obtain as raw materials and adopts classical elementary reactions such as cyclization, substitution, reduction and condensation, so that the flibanserin is prepared. The raw materials of the preparation method are easy to obtain, the technology is succinct, the yield is high, the preparation method is economical and environment-friendly, and a new preparation way is provided for the industrial production of the flibanserin.
Preparation method of flibaserin intermediate
-
Paragraph 0045; 0046; 0047; 0048; 0049, (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.
Method for industrial-scale efficient preparation of high-quality Flibaserin
-
Paragraph 0144; 0148, (2017/10/22)
The invention discloses a method for industrial-scale efficient preparation of high-quality Flibaserin, and belongs to the technical field of drug synthesis. The method comprises the following steps: A, putting benzimidazolone shown in Formula I and dihal