Electric Literature of 207346-42-7, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 207346-42-7, name is Methyl 2-amino-4,5-difluorobenzoate belongs to esters-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
To a solution of 70-1 (1.00 g, 5.34 mmol, 1 eq) and 70-lc (1.50 g, 8.02 mmol, 1.5 eq) in DCM (15 mL) were added Cu(OAc)2 (1.40 g, 8.02 mmol, 1.5 eq) and DIEA (1.30 g, 10.69 mmol, 1.8 mL, 2 eq). The mixture was degassed, purged with 02 for 3 times and stirred at 20C for 16 hr. The mixture was concentrated. The residue was dissolved in EA (10 mL) and washed with H20 (3 mL *3). The combined organic layers were washed with brine (3 mL *3), dried over Na2S04, filtered and concentrated under reduced pressure. The residue was purified by flash silica gel chromatography to give 70-2 (650.0 mg, 1.96 mmol, 36.7% yield). 1H NMR (400 MHz, CDCl3) d 9.61 (br s, 1H), 7.79 (dd, 7 = 9.0, 11.1 Hz, 1H), 7.58 (d, J= 8.5 Hz, 2H), 7.25 (d, .7= 2.3 Hz, 1H), 7.10 (dd, 7= 6.9, 12.8 Hz, 1H), 3.92 – 3.88 (m, 3H)
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, Methyl 2-amino-4,5-difluorobenzoate, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; VIVACE THERAPEUTICS, INC.; KONRADI, Andrei W.; LIN, Tracy Tzu-Ling Tang; (559 pag.)WO2019/222431; (2019); A1;,
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