Electric Literature of 541-16-2, 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 541-16-2 as follows.
A mixture of di-tert-butyl malonate (4.3 g, 19.91 mmol, 1.99 equiv) and potassium carbonate (2.8 g, 20.29 mmol, 2.03 equiv) in N,N-dimethylformamide (30 mL) was stirred at 65 C. for 30 min A solution of methyl 4-(4-(chloromethyl)-5-methyloxazol-2-yl)benzoate (2.65 g, 10.00 mmol, 1.00 equiv) in N,N-dimethylformamide (5 mL) was then added dropwise with stiffing to the reaction mixture. The resulting solution was stirred at 65 C. overnight and then quenched with 60 mL of ice and water. The mixture was extracted with 2×50 mL of ethyl acetate. The combined organic layers was washed with 3×30 mL of brine, dried over anhydrous sodium sulfate and concentrated under vacuum to give 4.0 g (90%) of methyl 4-(4-(3-tert-butoxy-2-(tert-butoxycarbonyl)-3-oxopropyl)-5-methyloxazol-2-yl)benzoate as a light yellow solid. LC-MS: (ES, m/z): 446 [M+H]+, 390, 334, 272, 230, 115.
According to the analysis of related databases, 541-16-2, the application of this compound in the production field has become more and more popular.
Reference:
Patent; The Board of Trustees of the Leland Stanford Junior University; Auckland UniServices Limited; Ruga Corporation; Giaccia, Amato; Lai, Edwin; Razorenova, Olga; Chan, Denise; Hay, Michael Patrick; Bonnet, Muriel; Sun, Connie; Tabibiazar, Ray; Yuen, Po-wai; US2015/329503; (2015); A1;,
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