These common heterocyclic compound, 2613-32-3, name is 2-Chloro-4,5-difluoroaniline, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. name: 2-Chloro-4,5-difluoroaniline
1-Chlor-1-dimethylamino-2-methyl-1-propen (64.9 mg, 0.486 mmol) was added to a solution of trans-4-[(pyrazolo[1 ,5-a]pyrim idin-3-ylcarbonyl)am ino]cyclohexanecarboxylic acid (70.0 mg, 0.243 mmol) in dichloromethane (3.1 ml) and the mixture was stirred at roomtemperature for 30 mi Pyridine (59 p1, 0.0.73 mmol) and 2-chloro-4,5-difluoroaniline (39.7 mg, 0.243 mmol, GAS No 261 3-32-3) were added and the mixture was stirred over night at room temperature. For work-up, water was added and the reaction mixture was extracted with dichloromethane. Die organic phase was filtrated through a silicone filter, concentrated and the residue purified by preparative HPLG (Method 9) to yield the title compound (3.8 mg,4% yield).LG-MS (Method 2): R = 1 .10 mm; MS (ESIpos) m/z = 434.1 [M+H].1HNMR (400 MHz, DMSO-d6): 6 [ppm] = 9.62 (5, 1H), 9.32 (dd, 1H), 8.83 (dd, 1H), 8.58 (5,1H), 7.86-7.76 (m, 3H), 7.28 (dd, 1H), 3.90-3.76 (m, 1H), 2.12-1.91 (m, 4H), 1.66-1.50 (m,2H), 1.45-1.31 (m, 2H).
The synthetic route of 2-Chloro-4,5-difluoroaniline has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; EIS, Knut; ACKERMANN, Jens; WAGNER, Sarah; BUCHGRABER, Philipp; SUeLZLE, Detlev; HOLTON, Simon; BENDER, Eckhard; LI, Volkhart; LIU, Ningshu; SIEGEL, Franziska; LIENAU, Philip; BAIRLEIN, Michaela; VON NUSSBAUM, Franz; HERBERT,Simon; KOPPITZ, Marcus; (734 pag.)WO2016/177658; (2016); A1;,
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