Application of 914347-48-1, 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. 914347-48-1, name is 2-[4-(6-Amino-2-methylpyrimidin-4-yl)piperazin-1-yl]ethanol. A new synthetic method of this compound is introduced below.
General procedure: Scheme 1 compound 8 (180.0 mg, 0.636 mmol) and 2-[4-(6-amino-2-methyl- pyrimidin-4-yl)-piperazin-l-yl]-ethanol (180.0 mg, 0.763 mmol) were dissolved in anhydrous dioxane (8 mL) in a flask. To this flask were added t-BuONa (183.0 mg, 1.908 mmol), X- PHOS (60.6 mg, 0.127 mmol), Pd(dba)2 (36.6 mg, 0.0636 mmol) under nitrogen atmosphere. The mixture was stirred at 80 C under nitrogen atmosphere overnight. TLC showed the starting material was consumed completely. The reaction mixture was concentrated, the residue was purified by prep-HPLC to give Compound 5 (90.0 mg, yield: 29.0%>) as a white solid. 1H NMR (400 MHz, CDC13+ MeOD + D20): delta 8.43 (s, 1H, CH), 7.97 (s, 1H, ArH), 7.61-7.25 (m, 5H, ArH), 6.44 (s, 1H, ArH), 4.30 (q, J= 7.2 Hz, 2H, CH2), 3.65-3.59 (m, 6H, 3CH2), 2.56-2.53 (m, 6H, 3CH2), 2.41 (s, 3H, CH3), 1.38 (t, J= 7.2 Hz, 3H, CH3). EXAMPLE 7
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,914347-48-1, its application will become more common.
Reference:
Patent; MANNKIND CORPORATION; TOLERO PHARMACEUTICALS, INC.; ZENG, Qingping; FARIS, Mary; MOLLARD, Alexis; WARNER, Steven L.; FLYNN, Gary A.; WO2014/52365; (2014); A1;,
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