Electric Literature of 915087-25-1, 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. 915087-25-1, name is 4-Amino-2-fluoro-N-methylbenzamide belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
Example 30 4-({2-[4-(5-Chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-3-(pyridin-2-yl)propanoyl}amino)-2-fluoro-N-methylbenzamide (Racemate) 75 mg (0.168 mmol) of 2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-3-(pyridin-2-yl)propanoic acid hydrochloride (racemate) and 43 mg (0.252 mmol, 1.5 eq.) of 4-amino-2-fluoro-N-methylbenzamide were initially charged in 1.5 ml of pyridine, 159 mul (0.672 mmol, 50% in ethyl acetate, 4.0 eq.) T3P were added and the mixture was stirred at 50 C. for 3 h. The reaction mixture was purified by means of preparative HPLC (RP18 column, eluent: acetonitrile/water gradient with addition of 0.1% formic acid). The product fractions were combined, concentrated and filtered by means of a hydrogen carbonate cartridge. Yield: 23 mg (25% of theory). LC/MS [Method 1]: Rt=0.85 min; MS (ESIpos): m/z=560 (M+H)+, 1H-NMR (400 MHz, DMSO-d6): delta [ppm]=10.92 (s, 1H), 8.52-8.45 (m, 1H), 8.12-8.03 (m, 1H), 7.96 (d, 1H), 7.74-7.61 (m, 5H), 7.54 (s, 1H), 7.43 (dd, 1 H), 7.34 (d, 1H), 7.25-7.19 (m, 1H), 6.42 (s, 1H), 6.10 (dd, 1H), 3.76-3.65 (m, 2H), 3.63 (s, 3H), 2.77 (d, 3H).
The synthetic route of 4-Amino-2-fluoro-N-methylbenzamide has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; ROeHRIG, Susanne; JIMENEZ NUNEZ, Eloisa; SCHLEMMER, Karl-Heinz; TERSTEEGEN, Adrian; TELLER, Henrik; HILLISCH, Alexander; HEITMEIER, Stefan; SCHMIDT, Martina Victoria; STAMPFUss, Jan; (82 pag.)US2017/298052; (2017); A1;,
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