Reference of 950596-58-4,Some common heterocyclic compound, 950596-58-4, name is 2-Amino-4,5-bis(2-methoxyethoxy)benzonitrile, molecular formula is C13H18N2O4, 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.
Example 1 (0025) In a reaction flask, 2-amino-4,5-bis(2-methoxyethoxy)-benzonitrile (37.01 g, 0.139 mol) and acetonitrile (185 ml) were charged; 3-ethynylaniline hydrochloride (30.00 g, 0.195 mol), trifluoroacetic acid (17.43 g, 0.152 mol) and formamidine acetate (15.19 g, 0.145 mol) were added to the resultant mixture. The reaction mixture was brought to the reflux temperature of the solvent and maintained under such conditions for about fifteen hours. At the end of the reaction, the temperature was brought to about 25 C., the solvent was removed by distillation under vacuum and methylethylketone (430 ml) was added. The organic phase was washed with a saturated sodium bicarbonate solution (2×100 ml) and with water (2×100 ml). The collected organic phases were concentrated to residue by distillation under vacuum. (0026) The resultant raw product was suspended in ethyl acetate (450 ml) and a solution of hydrochloric acid at 37% (14.38 g, 0.145 mol) was added, maintaining the temperature at 15 C. for about thirty minutes. The resultant solid was filtered, washed and dried in oven under vacuum at 45 C. to give 36.02 g of Erlotinib HCl.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Amino-4,5-bis(2-methoxyethoxy)benzonitrile, its application will become more common.
Reference:
Patent; CERBIOS-PHARMA SA; BARATELLA, Marco; PALLANZA, Giuseppe; GABOARDI, Mauro; CASTALDI, Graziano; (7 pag.)US2016/115137; (2016); A1;,
Nitrile – Wikipedia,
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