Category: 1247885-40-0

Application of 1247885-40-0,Some common heterocyclic compound, 1247885-40-0, name is 2,3-Difluoro-5-nitrobenzonitrile, molecular formula is C7H2F2N2O2, 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.

5-amino-2,3-difluorobenzonitrile (0273) To a solution of 2,3-difluoro-5-nitrobenzonitrile (920 mg, 5.00 mmol) in acetonitrile (25 mL) was added iron powder (1.96 g, 35.10 mmol) and acetic acid (6.0 g, 99.91 mmol). The resulting mixture was stirred for 2 h at room temperature and the solid that formed in the reaction mixture were removed by filtration. The filtrate was diluted with water (100 mL) and the pH value of the mixture was adjusted to 8 with saturated sodium bicarbonate solution. The resulting mixture was extracted with ethyl acetate (150 mL×2) and the organic phases were combined, washed with brine and dried over sodium sulfate. The solvent was removed under reduced pressure and the residue was purified by a neutral alumina column with ethyl acetate in hexane (0% to 65% gradient) to yield 5-amino-2,3-difluorobenzonitrile as yellow solid (660 mg, 86%).

The synthetic route of 1247885-40-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Merck Patent GmbH; SHERER, Brian A.; KARRA, Srinivasa; XIAO, Yufang; (407 pag.)US2016/376283; (2016); A1;,
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Reference of 1247885-40-0, These common heterocyclic compound, 1247885-40-0, name is 2,3-Difluoro-5-nitrobenzonitrile, 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.

A solution of 2,3-difluoro-5-nitrobenzonitrile (35 mg, 0.19 mmol) in acetonitrile (2 mL) was cooled to 00C. Acetic acid (228 mg, 3.80 mmol) and iron filings (75 mg, 1.33 mmol) were added, and the mixture was stirred at room temperature for 2 h. The reaction mixture was filtered and the filtrate was concentrated to give the crude product which was purified by prep-TLC (PE : EA = 2 : 1) to give the title compound as a yellow solid. (14 mg, 48%); LC/MS: m/e = 155 (M+H)+.

Statistics shows that 2,3-Difluoro-5-nitrobenzonitrile is playing an increasingly important role. we look forward to future research findings about 1247885-40-0.

Reference:
Patent; SEPRACOR INC.; BURDI, Douglas; SPEAR, Kerry, L.; HARDY, Larry, Wendell; WO2010/114971; (2010); A1;,
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts