Electric Literature of 274693-26-4, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 274693-26-4, name is 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol. A new synthetic method of this compound is introduced below.
Under nitrogen, the reaction flask were added isopropylidene ticagrelor, N,N- diisopropylethylamine (2.30g, 17.8mmol) and tetrahydrofuran 10mL, stirring (1.00g, 1.78mmol) 5 C to clarification, cooled to -5 C ~ 0 C. 5ml of tetrahydrofuran was added dropwise to the reaction solution phosphorus oxychloride (2.72g, 17.7mmol), the reaction solution is controlled temperature 0 C~ 5 C, 10min dropwise addition, the reaction temperature 0 C ~ 5 C for 2h. Under nitrogen, the reaction solution was slowly added dropwise 20ml of methanol, 0 C ~ 5 C reaction 1h, warmed to 10 C~ 15 C reaction was continued for 1h. To the reaction was added dropwise 30ml of water, temperature 5 C ~ 15C, addition was complete, warmed to 25 C ~ 30 C reaction 1h. 60ml of ethyl acetate twice. The combined organic phase was washed with 30ml water and 30ml saturated brine the organic phase, the resulting organic phase was dried over anhydrous sodium sulfate 1g IH, suction filtered, the filtrate was distilled off under reduced pressure, to give as a white solid 1.01g, yield 90.11%.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,274693-26-4, 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol, and friends who are interested can also refer to it.
Reference:
Patent; Hefei Medical Engineering Pharmaceutical Co., Ltd.; Hefei Enruite Pharmaceutical Co., Ltd.; Nanjing Medical Engineering Pharmaceutical Co., Ltd.; He Guangwei; Chu Zhaoxing; He Jianxun; Xu Qinlong; Ye Wenfeng; Li Jiaming; Xu Yungen; Wei Ping; Zhu Qihua; Wang Kui; Mo Jiajia; (16 pag.)CN108623629; (2018); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia