Synthetic Route of 20781-20-8, 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 20781-20-8 as follows.
To a solution of ethyl (4aS)-l-(4-fluorophenyl)-6-oxo-4,5,7,8-tetrahydrobenzo[f]indazole-4a- carboxylate (lg) (3.16 g, 8.92 mmol) and (2,4-dimethoxyphenyl)methanamine (2.68 mL, 17.8 mmol) in DCE (40 mL) was added acetic acid (1.54 mL, 26.8 mmol). After the reaction was stirred at rt for 5 min and cooled down in an ice-bath, sodium triacetoxyborohydride (5.l0g, 24.1 mmol) was added in portions. 5 Minute later, the reaction solution was allowed to warm to rt and continued stirring for 30 min. The solution was quenched (sat. aq. NaHCCE) and extracted (EtOAc). The organic layers were washed (brine), dried (Na2SC>4) and concentrated under reduced pressure. The crude product was purified by silica gel chromatography (0%-75% EtO Ac/hexanes, a gradient elution) to provide the title compound (4a) (4.15 g, 92% yield) as an off-white solid m/z (ESI, +ve ion) = 506.3 [M+H]+
According to the analysis of related databases, 20781-20-8, the application of this compound in the production field has become more and more popular.
Reference:
Patent; ORIC PHARMACEUTICALS, INC.; DU, Xiaohui; EKSTEROWICZ, John; FANTIN, Valeria R.; REW, Yosup; SUN, Daqing; YE, Qiuping; ZHOU, Haiying; KAWAI, Hiroyuki; MOORE, Jared; PHAM, Johnny; WU, Kejia; ZHU, Liusheng; (116 pag.)WO2020/76999; (2020); A1;,
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