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. 459817-82-4, name is tert-Butyl 1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide, A new synthetic method of this compound is introduced below., Recommanded Product: 459817-82-4
tert-Butyl l,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide (2.76 g, 12.37 mmol) was added portionwise to ethyl 4-(2-chloro-5-methylpyrimidin-4-yl)-lH-imidazole-2-carboxylate (Intermediate 23; 3.0 g, 11.25 mmol), K2CO3 (4.66 g, 33.75 mmol) and 18-crown-6 ether (0.595 g, 2.25 mmol) in 1,4-dioxane (60 mL) at 100 C under air. The resulting solution was stirred at 100 C for 2 hours. The mixture was cooled, filtered and the resulting solid was washed with ethyl acetate. The filtrate was then concentrated under reduced pressure. The crude product was purified by flash silica chromatography, elution gradient 25 to 30% EtOAc in petroleum ether. Pure fractions were evaporated to dryness to afford ethyl 1 -(2- ((tert-butoxycarbonyl)amino)ethyl)-4-(2-chloro-5-methylpyrimidin-4-yl)-lH-imidazole-2- carboxylate (Intermediate 22; 3.20 g, 69.4%) as a white solid. H NMR (400 MHz, DMSO, 20.2 C) delta 1.25 (9H, s), 1.35 (3H, t), 2.62 (3H, s), 3.35 (2H, dd), 4.37 (2H, q), 4.49 (2H, t), 6.93 (1H, t), 8.18 (1H, s), 8.61 (1H, s). m/z (ES+), [M+H]+ = 410
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; ASTRAZENECA AB; WARD, Richard, Andrew; JONES, Clifford, David; SWALLOW, Steven; GRAHAM, Mark, Andrew; DOBSON, Andrew, Hornby; MCCABE, James, Francis; (223 pag.)WO2017/80979; (2017); A1;,
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