Electric Literature of 328-70-1, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 328-70-1 as follows.
A mixed solution of 3,5-bis(trifluoromethyl)phenyl bromide (22.0 g), (R)-3-hydroxypyrrolidine hydrochloride (9.23 g), palladium(II) acetate (0.84 g), (+/-)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (4.68 g) and cesium carbonate (73.4 g) in toluene (300 mL)-1,4-dioxane (100 mL) was stirred under an argon gas atmosphere at 80 C. for 16 hr. The solid was filtered off, and the filtrate was washed with saturated brine and water, dried over anhydrous sodium sulfate, and filtered. The filtrate was concentrated, and the residue was purified by silica gel column chromatography (petroleum ether:ethyl acetate 10:1-3:1) to give the title compound (13.7 g, yield 61%) as a white solid.1H-NMR (300 MHz, CDCl3) delta: 1.74 (br, 1H), 2.06-2.31 (m, 2H), 3.28-3.38 (m, 1H), 3.39-3.50 (m, 1H), 3.50-3.66 (m, 2H), 4.61-4.73 (m, 1H), 6.87 (s, 2H), 7.12 (s, 1H).
According to the analysis of related databases, 328-70-1, the application of this compound in the production field has become more and more popular.
Reference:
Patent; Kasai, Shizuo; Kamaura, Masahiro; Cho, Nobuo; US2011/251187; (2011); A1;,
Bromide – Wikipedia,
bromide – Wiktionary