Reference of 5345-47-1, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.5345-47-1, name is 2-Aminonicotinic acid, molecular formula is C6H6N2O2, molecular weight is 138.12, as common compound, the synthetic route is as follows.
Example 1 – Synthesis of 2,4-dichloro-[1 ,8]naphthyridine; slurry of 4.90 kg (34.5 mol) 2-aminonicotinic acid in 50 I ethanol was treated with5.67 I (106 mol) sulfuric acid (98%). The reaction mixture was stirred for 60 hours at 79 C. The reaction mixture was then cooled to 40C and ethanol was distilled off under vacuum. The residue was dissolved in a mixture of 45 kg ice and 55 I water. Then 13 I aqueous sodium hydroxide solution (32% by weight) was added slowly under stirring and external cooling to reach a pH of 7. The precipitate was filtered off and washed with water. The residue was taken up in water, stirred for 1 hour and filtered. The residue was washed with water and dried under vacuum yielding 2- amino-nicotinic acid ethyl ester as colourless crystals; HPLC/MS: 0.99 min, [M+H] 167.1H NMR (400 MHz, DMSO) delta = 8.22 (dd, J=4.7, 2.0, 1 H), 8.07 (dd, J=7.8, 1.9, 1 H), 7.17 (s, 2H), 6.64 (dd, J=7.8, 4.7, 1 H), 4.29 (q, J=7.1 , 2H), 1 .32 (t, J=7.1 , 3H).
The chemical industry reduces the impact on the environment during synthesis 5345-47-1, I believe this compound will play a more active role in future production and life.
Reference:
Patent; MERCK PATENT GMBH; DORSCH, Dieter; JONCZYK, Alfred; HOELZEMANN, Guenter; AMENDT, Christiane; ZENKE, Frank; WO2012/595; (2012); A1;,
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