Aniracetam literature
Preparation method of aniracetam
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Paragraph 0018; 0042-0055, (2019/04/04)
The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of aniracetam. According to the preparation method of the aniracetam provided by the invention, a mixed acid anhydride intermediate is firstly generated by p-methoxybenzoic acid and pivaloyl chloride, and then the mixed acid anhydride intermediate reacts with 2-pyrrolidone to form a targetproduct, namely aniracetam. Therefore, the preparation method of the aniracetam has the advantages that the reaction steps are short, the reaction yield and the product purity are relatively high, rawmaterials are low in cost and easy to obtain, the operation is simple, and the method is suitable for large-scale industrial production and the like.
A Unified Strategy for the Synthesis of Difluoromethyl- And Vinylfluoride-Containing Scaffolds
Duchemin, Nicolas,Buccafusca, Roberto,Daumas, Marc,Ferey, Vincent,Arseniyadis, Stellios
supporting information, p. 8205 - 8210 (2019/10/16)
Here, we report a general method for the synthesis of quaternary and tertiary difluoromethylated compounds and their vinylfluoride analogues. The strategy, which relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and either a palladium-catalyzed decarboxylative protonation or a Krapcho decarboxylation, is practical, scalable, and high yielding. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.
Method for catalytically oxidizing amine to be synthesized into amide through dipyridyl-type manganese catalyst
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Paragraph 0017-0027; 0052-0054, (2019/06/30)
The invention discloses a methodfor catalytically oxidizing amine to be synthesized into amide througha dipyridyl-type manganese catalyst. According to the method, a dipyridyl manganese complex formedafter coordination of a dipyridyl-type complex and cheap metal manganese serves as the catalyst, clean and environment-friendly hydrogen peroxide serves as an oxidizing agent, oxidation of N ortho-position sp3 C-H bonds catalyzed by the cheap metal manganese is achieved, and the amine is directly oxidized to obtain the amide. Compared with existing methods, the method has the advantages that theadopted catalyst is low in price, the preparing method is simple, raw materials are easy to obtain, the use level of the catalyst is low, the substrate range is wide, the reaction condition is mild, the operation is simple and environmentally friendly, the reaction time is short, the yield is high, the selectivity is high, and the industrialization cost is low.
Catalytic synthesis method of Aniracetam
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Paragraph 0058; 0059; 0061; 0062; 0063-0073, (2019/05/08)
The invention belongs to the technical field of drug synthesis, and in particular relates to a catalytic synthesis method of Aniracetam. The catalytic synthesis method comprises the steps as follows:adding an organic solvent, p-methoxybenzoic acid, 2-pyrrolidone and a boric acid catalyst into a reaction vessel, reacting completely, and performing post-treatment to obtain Aniracetam. The catalyticeffect of the boric acid catalyst is remarkable, and the catalyst itself is cheap and easily available, thereby producing high economic efficiency. The catalytic synthesis method has high atomic utilization rate, and the by-product produced by the method is water, which causes no pollution to the environment. The catalytic synthesis method is easy to operate, and the reaction yield and product purity are high. In summary, the catalytic synthesis method of Aniracetam adopts a green environmentally-friendly preparation process, which is low-cost and especially suitable for large-scale industrial production. Thereby, the method of the invention has a broad application prospect and good market potential.