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. 1209459-32-4, name is 4-(2-Bromopyrimidin-4-yl)morpholine. A new synthetic method of this compound is introduced below., category: pyrimidines
To a microwave vi charged with (S)-2-(3,4-dimethylpiperazin-l-yl)-4-fluoro-5-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2-yl)aniline (0.143, 0.410 mmol), 4-(2-bromopyrimidin-4-yl)morpholine (0.150 g ,0.615 mmol), K3P04 (0.174 g, 0.819 mmol) was added dioxane (2 ml) and water (2 ml) and the vial was flushed with nitrogen. Bis(di-tert-butyl(4-dimethylaminophenyl)phosphine)dichloropalladium(II) (0.0087 g, 0.030 mmol) was added, the vial was sealed, and the mixture heated in a microwave reactor to 110C for 30 minutes. The crude mixture was concentrated onto celite and purified using reverse phase silca gel column chromatography (Water: AcCN gradient 0-100%). The product was dried under vacuum to give the title compound as a brown solid (0.097 g, 61 %); LCMS [M + H]+ 387
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Reference:
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ZEPEDA-VELAZQUEZ, Carlos Armando; PODA, Gennady; ISAAC, Methvin; UEHLING, David; WILSON, Brian; JOSEPH, Babu; LIU, Yong; SUBRAMANIAN, Pandiaraju; MAMAI, Ahmed; PRAKESCH, Michael; STILLE, Julia Kathleen; (1053 pag.)WO2017/147700; (2017); A1;,
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