Synthetic Route of 129768-28-1, 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 129768-28-1 as follows.
General procedure: To a mixture of D-a (100 mg, 0.46 mmol), acid (0.56 mmol), HATU (262 mg, 0.69 mmol) and N, /V-diisopropylethylamine (118 mg, 0.92 mmol) i n N, A’-d i m e th y 1 fo rm am i dc (3 mL) was stirred at 25 C for 2-24 h. The mixture was diluted by the addition of water, followed by General Work-up Procedure 1. The residue was purified by prep-HPLC or flash column chromatography to afford the desired product. The amide bond formation reaction was carried out in a similar fashion as for 184 using 3-(trifluoromcthyl)- l//-pyrazolc-5-carboxylic acid (61 mg, 0.34 mmol, 1.5 eq.) and D-a (50 mg, 0.23 mmol, 1 eq.) as reactants afforded the title compound (trifluoroacetic acid salt, 63 mg, 56%) as an off-white solid: 1H NMR (500 MHz, DMSO-ri6) 14.58 (d, J = 32.8 Hz, 1H), 10.26 (s, 1H), 8.78 (s, 1H), 7.54 (s, 2H), 7.47 (s, 1H), 7.25 (t, J = 7.8 Hz, 1H), 7.03 – 6.97 (m, 1H), 3.52 (s, 3H), 3.22 (h, J = 6.8 Hz, 1H), 3.12 – 3.02 (m, 2H), 1.25 (d, J = 6.9 Hz, 3H); LCMS: C17H17F3N6O requires: 378, found: m/z = 379 [M+H]+.
According to the analysis of related databases, 129768-28-1, the application of this compound in the production field has become more and more popular.
Reference:
Patent; NURIX THERAPEUTICS, INC.; BARSANTI, Paul A.; BENCE, Neil F.; GOSLING, Jennifa; SAHA, Anjanabha; TAHERBHOY, Asad M.; ZAPF, Christoph W.; BOYLE, Kathleen; CARDOZO, Mario; MIHALIC, Jeffrey; LAWRENZ, Morgan; GALLOP, Mark; BRUFFEY, Jilliane; CUMMINS, Thomas; ROBBINS, Daniel; TANAKA, Hiroko; WANG, Chenbo; COHEN, Frederick; PALMER, Wylie; SANDS, Arthur T.; SHUNATONA, Hunter; (968 pag.)WO2019/148005; (2019); A1;,
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