Application of 62802-42-0, 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. 62802-42-0, name is 2-Chloro-5-fluoropyrimidine. A new synthetic method of this compound is introduced below.
A solution of N- [(4aR,7a5)-7a-(2-fluorophenyl)-4a,5 ,6,7-tetrahydro-4H- pyrrolo[3,4-dl[1,3lthiazin-2-yllbenzamide (124.7 g, 256 mmol), DIPEA (67 mL), 5- fluoro-2-chloropyrimidine (29.3 ml, 307 mmol) in N-methylpyrrolidone (997 mL) isheated to 100 C for 16 hours. The reaction is cooled to 22 C and poured into cooled water at 10 C (10 L) keeping temperature below 15 C. A pale cream solid is collected by filtration and washed with additional water. The wet solid is dissolved in EtOAc (2 L) and transferred to a separator funnel. Sodium chloride aqueous solution 5% w/w (1 L) is added and the organic layer is separated, dried over sodium sulfate, filtered, and the filtrate evaporated under reduced pressure. The product is purified by silica gel chromatography using a gradient of 0-40% EtOAc/isohexane to give the title compound as a pale yellow solid (116 g, 70%). ES/MS (mlz): 452 (M+H).
At the same time, in my other blogs, there are other synthetic methods of this type of compound,62802-42-0, 2-Chloro-5-fluoropyrimidine, and friends who are interested can also refer to it.
Reference:
Patent; ELI LILLY AND COMPANY; COATES, David Andrew; WOLFANGEL, Craig Daniel; (55 pag.)WO2016/122968; (2016); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia