326-62-5Relevant articles and documents
Rapid and Simple Access to α-(Hetero)arylacetonitriles from Gem-Difluoroalkenes
Hu, Dandan,Liu, Jiayue,Ren, Hongjun,Song, Jinyu,Zhang, Jun-Qi,Zhu, Guorong
supporting information, p. 786 - 790 (2022/01/28)
A scalable cyanation of gem-difluoroalkenes to (hetero)arylacetonitrile derivatives was developed. This strategy features mild reaction conditions, excellent yields, wide substrate scope, and broad functional group tolerance. Significantly, in this reacti
Synthetic method of prasugrel intermediate o-fluorophenylacetic acid
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Paragraph 0029; 0032-0036; 0038; 0041-0045; 0047; 0050-0054, (2020/02/19)
The invention discloses a synthetic method of prasugrel intermediate o-fluorophenylacetic acid. The reaction process comprises the steps that (1) 2-fluorotoluene, N-halosuccinimide, an initiator and asolvent S1 are mixed uniformly, protective gas is introduced, the pressure is controlled to be 1.5-2 atmospheric pressure, the temperature is controlled to be 90-120 DEG C, stirring reaction is conducted for 1-2 h, and a mixture M1 is obtained; (2) a catalyst is mixed uniformly with a cyanide aqueous solution, the pressure is controlled to be 2-3 atmospheric pressure, the temperature is controlled to be 80-100 DEG C, the mixture M1 is added into a reaction system, then conditions are maintained to continue the reaction for 1-2 h, still standing and layering are conducted, organic phase is collected and concentrated to 1/2 of the original volume, and a mixture M2 is obtained; and (3) the mixture M2 is mixed uniformly with hydrochloric acid and glacial acetic acid, refluxing is conducted for 40-55 min, the mixture is poured into crushed ice after cooling, a solvent S2 is added for extraction, and after the organic phase is dried by a drying agent, a product is obtained by concentratingby a rotary evaporator. According to the synthetic method, safety and reliability are achieved, the production cost is low, three wastes are basically avoided, and the synthetic method is suitable forindustrial production.
Efficient synthesis of prasugrel, a novel P2Y12 receptor inhibitor
Pan, Xianhua,Huang, Rui,Zhang, Jianshui,Ding, Liping,Li, Weijin,Zhang, Qunhui,Liu, Feng
, p. 5364 - 5366 (2012/10/29)
An efficient synthesis of prasugrel, a novel P2Y12 receptor inhibitor, is described. The cyclopropyl-phenylethanone intermediate was prepared by cyanide substitution, bromination, N-substitution, and the Grignard reaction. After acid hydrolyzation of the methyl ether and subsequent acetylation, the title product was obtained with a total yield of 21% after 10 linear steps from simple and commercially available raw materials.
