In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 959236-97-6, name is 4-Bromo-2-(methylthio)pyrimidine, the common compound, a new synthetic route is introduced below. category: pyrimidines
step 1: A suspension of 4-bromo-2-(methylthio)pyrimidine (7.00 g, 34.1 mmol), 2-fluoropyridin- 4-ylboronic acid (5.05 g, 35.8 mmol), Na2C03 (10.9 g, 102 mmol) and Pd(dppf)Cl2 CH2C12 (1.40 g, 1.71 mmol) in dioxane/H20 (100 mL; 1:1) was heated to 85C under an Ar balloon for 2 h. The reaction mixture was cooled to RT and concentrated. The residue was diluted with ethyl acetate (200 mL) and water (100 mL). The layers were separated, and the aqueous layer was extracted with ethyl acetate (IX). The organics were dried, filtered and concentrated. The crude product was purified via column chromatography, eluting with hexanes/ethyl acetate (3: 1) to give 4-(2-fluoropyridin-4-yl)-2-(methylthio)pyrimidine (6.83 g, 90%) as a solid. XH NMR (400 MHz, (CD3)2SO) delta 8.85 (d, J=5.2 Hz, 1H), 8.46 (d, J=5.2 Hz, 1H), 8.11 (m, 1H), 7.96 (d, J=5.2 Hz, 1H), 7.92 (s, 1H), 2.62 (s, 3H); m/z (APCI-pos) M+l = 222.1.
The synthetic route of 959236-97-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; BELVIN, Marcia; MOFFAT, John; MERCHANT, Mark; WO2015/32840; (2015); A1;,
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